Synthesis and antiproliferative activity of new cytotoxic azanaphthoquinone pyrrolo-annelated derivatives: Part II (Englisch)

In: Bioorganic and Medicinal Chemistry Letters   ;  21 ,  10  ;  3117-3121  ;  2011
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Graphical abstract

Abstract A series of 6-azanaphthoquinone pyrrolo-annelated derivatives carrying different basic side chains have been synthesized. The antiproliferative activities of all compounds were evaluated on at least four different cell lines with Mitoxantrone as reference compound. Cytotoxic effects and DNA intercalation behavior were investigated.

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9
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9
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Czalkowski, D.P. / Reddy, A.V.N. / Setti, E.L. / Phillips, O.A. / Micetich, R.G. / Kunugita, C. / Maiti, S.N. | 1997
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11
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Czajkowski, D. P. / Reddy, A. V. N. / Setti, E. L. / Phillips, O. A. / Micetich, R. G. / Kunugita, C. / Maiti, S. N. | 1997
11
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Zhurilo, Nikolay I. / Chudinov, Mikhail V. / Matveev, Andrey V. / Smirnova, Olga S. / Konstantinova, Irina D. / Miroshnikov, Anatoly I. / Prutkov, Alexander N. / Grebenkina, Lyubov E. / Pulkova, Natalya V. / Shvets, Vitaly I. | 2018
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13
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| 2004
13
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13
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Palumbo, Anna / Napolitano, Alessandra / d'Ischia, Marco | 2002
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Hiraoka, Takashi / Hamachi, Itaru | 2002
13
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Shen, Z.-J. / Kim, S. K. / Lee, Y. S. / Lee, J. W. / Moon, B. J. | 1999
13
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Shen, Z.-J. / Kim, S.K. / Lee, Y.S. / Lee, J.W. / Moon, B.J. | 1999
13
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Crombie, Leslie / Josephs, Jonathan L. / Cayley, Jane / Larkin, John / Weston, John B. | 1991
13
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Cocker, J.D. / Davies, H.G. | 1996
15
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15
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Ohfune, Yasufumi / Shimamoto, Keiko / Ishida, Michiko / Shinozaki, Haruhiko | 1993
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15
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Arai, T. / Shinozuka, K. / Sawai, H. | 1997
15
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15
Foreword
Greenlee, W.J. / Mantlo, N.B. | 1994
15
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Ohfune, Y. / Shimamoto, K. / Ishida, M. / Shinozaki, H. | 1993
15
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15
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15
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15
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16
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17
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| 2006
17
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Mantlo, Nathan B. / Kim, Dooseop / Ondeyka, Debra / Chang, Raymond S.L. / Kivlighn, Salah D / Siegl, Peter K.S. / Greenlee, William J. | 1993
17
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17
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17
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Steele, T. G. / Hills, I. D. / Nomland, A. A. / de Leon, P. / Allison, T. / McGaughey, G. / Colussi, D. / Tugusheva, K. / Haugabook, S. J. / Espeseth, A. S. | 2009
17
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17
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17
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Kadow, John F. / Tun, Min Min / Crosswell, Alfred R. / Rose, William C. / Vyas, Dolatrai M. / Doyle, Terrence W. | 1991
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Mederskl, W.W.K.R. / Osswald, M. / Dorsch, D. / Anzall, S. / Christadler, M. / Schmitges, C.-J. / Wilm, C. | 1998
17
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Cunningham, B.R. / Rivetna, M. / Tolman, R.L. / Flattery, S.J. / Nichols, E.A. / Schwartz, C.D. / Wicker, L.S. / Hermes, J.D. / Jones, A.B. | 1997
19
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| 2003
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19
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Whitten, J.P. / Cube, R.V. / Baron, B.M. / McDonald, I.A. | 1993
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Kawasaki, N. / Miyataka, H. / Matsumoto, H. / Yamashita, N. / Sakane, T. / Mizushima, Y. / Satoh, T. | 1999
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Hill, D.T. / Girard, G.R. / Weinstock, J. / Edwards, R.M. / Weidley, E.F. / Ohlstein, E. / Peishoff, C.E. / Baker, E. / Aiyar, N. | 1995
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Campestre, Cristina / Agamennone, Mariangela / Tortorella, Paolo / Preziuso, Serena / Biasone, Alessandro / Gavuzzo, Enrico / Pochetti, Giorgio / Mazza, Fernando / Hiller, Oliver / Tschesche, Harald et al. | 2005
20
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Ramsey, Deborah M. / McAlpine, Shelli R. | 2012
21
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Gargano, Emanuele Marco / Perspicace, Enrico / Carotti, Angelo / Marchais-Oberwinkler, Sandrine / Hartmann, Rolf W. | 2015
21
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Stevens, Kirk L. / Alligood, Krystal J. / Alberti, Jennifer G. Badiang / Caferro, Thomas R. / Chamberlain, Stanley D. / Dickerson, Scott H. / Dickson, Hamilton D. / Emerson, Holly K. / Griffin, Robert J. / Hubbard, Robert D. et al. | 2008
21
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Kinoshita, Takayoshi / Nakanishi, Isao / Sato, Akihiro / Tada, Toshiji | 2002
21
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Munchhof, Michael J. / Beebe, Jean S. / Casavant, Jeffery M. / Cooper, Beth A. / Doty, Jonathan L. / Higdon, R.Carla / Hillerman, Stephen M. / Soderstrom, Catherine I. / Knauth, Elisabeth A. / Marx, Matthew A. et al. | 2003
21
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Santagada, Vincenzo / Caliendo, Giuseppe / Severino, Beatrice / Perissutti, Elisa / Fiorino, Ferdinando / Cicala, Carla / De Filippis, Vincenzo / Cirino, Giuseppe | 2002
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23
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23
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23
Synthesis of biologically active dihydrodiol metabolites of 16,17-dihydro-15H-cyclopenta[a]phenanthrene and its carcinogenic 11-methyl and 17-keto derivatives
Young, Robert J. / Cortez, Cecilia / Luna, Ernestina / Lee, H. / Harvey, Ronald G. | 1991
23
Hydroxamate-based inhibitors of low affinity IgE receptor (CD23) processing
Balley, S. / Bolognese, B. / Buckle, D.R. / Faller, A. / Jackson, S. / Louis-Flamberg, P. / McCord, M. / Mayer, R.J. / Marshall, L.A. / Smith, D.G. | 1998
23
Beneficial effects of different flavonoids, on functional recovery after ischemia and reperfusion in isolated rat heart
Lebeau, Jonathan / Neviere, Rémi / Cotelle, Nicole | 2001
23
Competitive NMDA receptor antagonists; (R)-4-Oxo-5-phosphononorvaline structure-activity relationships
Whitten, Jeffrey P. / Baron, Bruce M. / McDonald, Ian A. | 1993
23
Anti HIV-1 activity of a hydrophilic cyclosporin derivative with improved binding affinity to cyclophilin A
Papageorgiou, C. / Sanglier, J.-J. / Traber, R. | 1996
24
Synthesis and in vitro evaluations of 6-(hetero)-aryl-imidazo[1, 2-b]pyridazine-3-sulfonamide's as an inhibitor of TNF-α production
Pandit, Shivaji S. / Kulkarni, Mahesh R. / Pandit, Yashwant B. / Lad, Nitin P. / Khedkar, Vijay M. | 2018
24
Design and synthesis of 4,5,6,7‐tetrahydro‐1H‐1,2‐diazepin‐7‐one derivatives as a new series of Phosphodiesterase 4 (PDE4) inhibitors
Guariento, Sara / Karawajczyk, Anna / Bull, James A. / Marchini, Gessica / Bielska, Martyna / Iwanowa, Xenia / Bruno, Olga / Fossa, Paola / Giordanetto, Fabrizio | 2016
25
3-Methoxycarbonyl-5-nitrophenyl boronic acid: high affinity diol recognition at neutral pH
Mulla, Hormuzd R. / Agard, Nicholas J. / Basu, Amit | 2003
25
Synthesis and multiparametric evaluation of thiadiazoles and oxadiazoles as diacylglycerol acyltransferase type 1 inhibitors
Mougenot, Patrick / Namane, Claudie / Fett, Eykmar / Goumy, Florence / Dadji-Faïhun, Rommel / Langot, Gwladys / Monseau, Catherine / Onofri, Bénédicte / Pacquet, François / Pascal, Cécile et al. | 2015
25
Insight into reduction of obacunone, and their ester derivatives as insecticidal agents against Mythimna separata Walker
Yu, Xiang / Ding, Guodong / Zhi, Xiaoyan / Xu, Hui | 2014
25
Nonpeptide avb3 antagonists. Part 2: constrained glycyl amides derived from the RGD tripeptide
Meissner, Robert S. / Perkins, James J. / Duong, Le T. / Hartman, George D. / Hoffman, William F. / Huff, Joel R. / Ihle, Nathan C. / Leu, Chih-Tai / Nagy, Rose M. / Naylor-Olsen, Adel et al. | 2002
25
Modulators of the human CCR5 receptor. Part 1: Discovery and initial SAR of 1-(3,3-diphenylpropyl)-piperidinyl amides and ureas
Burrows, Jeremy N. / Cumming, John G. / Fillery, Shaun M. / Hamlin, Gordon A. / Hudson, Julian A. / Jackson, Ruth J. / McLaughlin, Sharon / Shaw, John S. | 2004
25
The synthesis and biological activity of some known and putative metabolites of the atypical antipsychotic agent olanzapine (LY170053)
Calligaro, D. O. / Fairhurst, J. / Hotten, T. M. / Moore, N. A. / Tupper, D. E. | 1997
25
The synthesis and biological activity of some known and putative metabolites and of the atypical antipsychotic agent olanzapine (LY170053)
Calligaro, D.O. / Fairhurst, J. / Hotten, T.M. / Moore, N.A. / Tupper, D.E. | 1997
25
Identification of a stable chymase inhibitor using a pharmacophore-Based database search
Koide, Yuuki / Tatsui, Akira / Hasegawa, Takeshi / Murakami, Akira / Satoh, Shoji / Yamada, Hideki / Kazayama, Shin-ichi / Takahashi, Atsuo | 2002
25
Development and evaluation of a pharmacophore model for inhibitors of aldosterone synthase (CYP11B2)
Ulmschneider, Sarah / Negri, Matthias / Voets, Marieke / Hartmann, Rolf W. | 2005
25
Inhibitors of the adenovirus type 2 proteinase based on substrate-like tetrapeptide nitriles
Cornish, J.A. / Murray, H. / Kemp, G.D. / Gani, D. | 1995
25
Synthesis and methemoglobin toxicity of the amides of 6-7 mono or disubstituted quinolone
Srivastava, S. / Srivastava, S.K. / Shukla, A. / Chauhan, P.M.S. / Puri, S.K. / Bhaduri, A.P. / Pandey, V.C. | 1999
26
Exploring SAR features in diverse library of 4-cyanomethyl-pyrazole-3-carboxamides suitable for further elaborations as CB1 antagonists
Cooper, Martin / Receveur, Jean-Marie / Bjurling, Emelie / Nørregaard, Pia K. / Nielsen, Peter Aadal / Sköld, Niklas / Högberg, Thomas | 2009
26
Fluorescent ligands for adenosine receptors
Kozma, Eszter / Suresh Jayasekara, P. / Squarcialupi, Lucia / Paoletta, Silvia / Moro, Stefano / Federico, Stephanie / Spalluto, Giampiero / Jacobson, Kenneth A. | 2012
27
Enzymatic asymmetric synthesis of (2R,4R,5S)-2-amino-4,5-(1,2-cyclohexyl)-7-phosphonohetanoic acid, a potent, selective and competitive NMDA antagonist
Hamilton, G.S. / Huang, Z. / Patch, R.J. / Narayanan, B.A. / Ferkany, J.W. | 1993
27
Discovery of potent, selective sulfonylfuran urea endothelial lipase inhibitors
Goodman, Krista B. / Bury, Michael J. / Cheung, Mui / Cichy-Knight, Maria A. / Dowdell, Sarah E. / Dunn, Allison K. / Lee, Dennis / Lieby, Jeffrey A. / Moore, Michael L. / Scherzer, Daryl A. et al. | 2008
27
6-Acylamino-2-((alkylsulfonyl)oxy)-1H-isoindole-1,3-dione mechanism-based inhibitors of human leukocyte elastase
Kerrigan, John E. / Walters, Matthew C. / Forrester, Kerri J. / Crowder, Jason B. / Christopher, Lisa J. | 2000
27
Selectively deoxygenated sulfated tetrasaccharides as probes for the investigation of smooth muscle cell antiproliferative activity
Wessel, H.P. / Iberg, N. / Trumtel, M. / Viaud, M.-C. | 1996
27
Enzymatic asymmetric synthesis of (2R, 4R, 5S)-2-amino-4,5-(1,2-cyclohexyl)-7-phosphonoheptanoic acid, a potent, selective and competitive NMDA antagonist
Hamilton, G.S. / Huang, Z. / Patch, R.J. / Narayanan, B.A. / Ferkany, J.W. | 1993
27
Synthesis and biological activity of C-6 modified derivatives of the glucosidase inhibitor 1-deoxynojirimycin.
Berger, A. / Dax, K. / Gradnig, G. / Grassberger, V. / Stütz, A.E. / Ungerank, M. / Legler, G. / Bause, E. | 1991
28
Structure and property based design of factor Xa inhibitors: Biaryl pyrrolidin-2-ones incorporating basic heterocyclic motifs
Young, Robert J. / Borthwick, Alan D. / Brown, David / Burns-Kurtis, Cynthia L. / Campbell, Matthew / Chan, Chuen / Charbaut, Marie / Convery, Máire A. / Diallo, Hawa / Hortense, Eric et al. | 2007
28
Isothiazoles as active-site inhibitors of HCV NS5B polymerase
Yan, Shunqi / Appleby, Todd / Gunic, Esmir / Shim, Jae Hoon / Tasu, Tania / Kim, Hongwoo / Rong, Frank / Chen, Huaming / Hamatake, Robert / Wu, Jim Z. et al. | 2006
28
Seco-4-methyl-DCK derivatives as potent chemosensitizers
Guo, Yalan / Wang, Ke / Chen, Xiaoyu / Li, Haihong / Wan, Qi / Morris-Natschke, Susan / Lee, Kuo-Hsiung / Chen, Ying | 2019
29
5-Amidinobenzo[b]thiophenes as dual inhibitors of factors IXa and Xa
Qiao, Jennifer X. / Cheng, Xuhong / Modi, Dilip P. / Rossi, Karen A. / Luettgen, Joseph M. / Knabb, Robert M. / Jadhav, Prabhakar K. / Wexler, Ruth R. | 2004
29
Valsartan, a potent, orally active angiotensin II antagonist developed from the structurally new amino acid series
Bühlmayer, Peter / Furet, Pascual / Criscione, Leoluca / de Gasparo, Marc / Whitebread, Steven / Schmidlin, Tibur / Lattmann, René / Wood, Jeanette | 1993
29
New orally active PDE4 inhibitors with therapeutic potential
Ochiai, Hiroshi / Ishida, Akiharu / Ohtani, Tazumi / Kusumi, Kensuke / Kishikawa, Katuya / Obata, Takaaki / Nakai, Hisao / Toda, Masaaki | 2003
29
Inhibition of BCRP-mediated drug efflux by fumitremorgin-type indolyl diketopiperazines
van Loevezijn, Arnold / Allen, John D. / Schinkel, Alfred H. / Koomen, Gerrit-Jan | 2001
29
Selective inhibition of low affinity IgE receptor (CD23) processing
Bailey, S. / Bolognese, B. / Buckle, D.R. / Faller, A. / Jackson, S. / Louis-Flamberg, P. / McCord, M. / Mayer, R.J. / Marshall, L.A. / Smith, D.G. | 1998
30
Modification of amphipathic non-opioid dynorphin A analogues for rat brain bradykinin receptors
Lee, Yeon Sun / Hall, Sara M. / Ramos-Colon, Cyf / Remesic, Michael / LeBaron, Lindsay / Nguyen, Ann / Rankin, David / Porreca, Frank / Lai, Josephine / Hruby, Victor J. | 2014
30
Utilization of alkyne bioconjugations to modulate protein function
Maza, Johnathan C. / Howard, Christina A. / Vipani, Megha A. / Travis, Christopher R. / Young, Douglas D. | 2016
31
Design, synthesis and in vitro antimalarial activity of an acylhydrazone library
Melnyk, Patricia / Leroux, Virginie / Sergheraert, Christian / Grellier, Philippe | 2005
31
Reaction of reductively activated mitomycin C with aqueous bicarbonate: Isolation and characterization of an oxazolidinone derivative of cis-1-hydroxy-2,7-diaminomitosene
Paz, Manuel M. | 2009
31
2,3-Substituted 2-azanorbomanes as polar b-turn mimetics
Horwell, D.C. / Naylor, D. / Willems, H.M.G. | 1997
31
New minimal substrate structural requirements in the enzymatic peroxidation of alkenes with soybean lipoxygenase
Novak, M.J. | 1999
31
Discovery of a-amidosulfones as potent and selective agonists of CB2: Synthesis, SAR, and pharmacokinetic properties
Marx, I. E. / DiMauro, E. F. / Cheng, A. / Emkey, R. / Hitchcock, S. A. / Huang, L. / Huang, M. Y. / Human, J. / Lee, J. H. / Li, X. | 2009
31
Discovery of 5-((5-chloro-2-methoxyphenyl)sulfonamido)nicotinamide (SBI-425), a potent and orally bioavailable tissue-nonspecific alkaline phosphatase (TNAP) inhibitor
Pinkerton, Anthony B. / Sergienko, Eduard / Bravo, Yalda / Dahl, Russell / Ma, Chen-Ting / Sun, Qing / Jackson, Michael R. / Cosford, Nicholas D.P. / Millán, José Luis | 2018
31
Non-Peptide avb3 antagonists. Part 3: Identification of potent RGD mimetics incorporating novel b-Amino acids as aspartic acid replacements
Coleman, Paul J. / Brashear, Karen M. / Hunt, Cecilia A. / Hoffman, William F. / Hutchinson, John H. / Breslin, Michael J. / Mcvean, Carol A. / Askew, Ben C. / Hartman, George D. / Rodan, Sevgi B. et al. | 2002
31
Discovery of α-amidosulfones as potent and selective agonists of CB2: Synthesis, SAR, and pharmacokinetic properties
Marx, Isaac E. / DiMauro, Erin F. / Cheng, Alan / Emkey, Renee / Hitchcock, Stephen A. / Huang, Liyue / Huang, Ming Y. / Human, Jason / Lee, Josie H. / Li, Xingwen et al. | 2008
31
Siphonols A–E: Novel nitric oxide inhibitors from Orthosiphon stamineus of Indonesia
Awale, Suresh / Tezuka, Yasuhiro / Banskota, Arjun H. / Kadota, Shigetoshi | 2002
31
The utilization of a unified pharmacophore query in the discovery of new antagonists of the adenosine receptor family
Webb, Thomas R. / Melman, Neli / Lvovskiy, Dmitriy / Ji, Xiao-duo / Jacobson, Kenneth A. | 2000
31
2,3-Substituted 2-azanorbornanes as polar �-turn mimetics
Horwell, D. C. / Naylor, D. / Willems, H. M. G. | 1997
31
Synthesis of a new type of 5-deazaflavoquinone (hybrid model compound of 5-deazaflavin and coenzyme PQQ)
Kimachi, T. / Sugita, K. / Bessho, K. / Yoneda, F. | 1995
32
Targeting tyrosine kinase: Development of acridone – pyrrole – oxindole hybrids against human breast cancer
Kaur, Manpreet / Singh, Palwinder | 2019
33
New reagents for controlled release of nitric oxide. Structure-stability relationships
Kato, M. / Nishino, S. / Ohno, M. / Fukuyama, S. / Kita, Y. / Hirasawa, Y. / Nakanishi, I. / Takasugi, H. / Sakane, K. | 1996
33
Drug discovery considerations in the development of covalent inhibitors
Mah, Robert / Thomas, Jason R. / Shafer, Cynthia M. | 2013
33
Rational design, synthesis and in vitro evaluation of allylidene hydrazinecarboximidamide derivatives as BACE-1 inhibitors
Jain, Priti / Wadhwa, Pankaj K. / Rohilla, Shilpa / Jadhav, Hemant R. | 2015
33
Mechanism-based active site modification of the soybean sterol methyltransferase by 26,27-dehydrocycloartenol
Song, Zhihong / Zhou, Wenxu / Liu, Jialin / Nes, W.David | 2003
33
Pharmacology of (2R, 4R, 5S)-2-amino-4,5-(1,2-cyclohexyl)-7-phosphonoheptanoic acid (NPC 17742); a selective, systemically active, competitive NMDA antagonist
Ferkany, J.W. / Willetts, J.S.A. / Borosky, D.B. / Clissold, E.W. / Karbon / Hamilton, G.S. | 1993
33
Phthalazine PDE4 inhibitors. Part 2: The synthesis and biological evaluation of 6-methoxy-1,4-disubstituted derivatives
Napoletano, Mauro / Norcini, Gabriele / Pellacini, Franco / Marchini, Francesco / Morazzoni, Gabriele / Ferlenga, Pierpaolo / Pradella, Lorenzo | 2001
33
Pharmacology of (2R,4R,5S)-2-amino-4,5-(1,2-cyclohexyl)-7-phosphonoheptanoic acid (NPC 17742) a selective,systemlcally active, competitive NMDA antagonist
Ferkany, J.W. / Willetts, J. / Borosky, S.A. / Clissold, D.B. / Karbon, E.W. / Hamilton, G.S. | 1993
33
Azasugar and glycal inhibitors of α-L-fucosidase
Dumas, David P. / Kajimoto, Tetsuya / Liu, Kevin K.-C. / Wong, Chi-Huey / Berkowitz, David B. / Danieshefsky, Samuel J. | 1991
34
Amino acid derivatives as histone deacetylase inhibitors
Hubbs, Jed L. / Zhou, Hua / Kral, Astrid M. / Fleming, Judith C. / Dahlberg, William K. / Hughes, Bethany L. / Middleton, Richard E. / Szewczak, Alexander A. / Secrist, J. Paul / Miller, Thomas A. | 2007
34
Identification of potent and selective TACE inhibitors via the S1 pocket
Condon, Jeffrey S. / Joseph-McCarthy, Diane / Levin, Jeremy I. / Lombart, Henry-Georges / Lovering, Frank E. / Sun, Linhong / Wang, Weiheng / Xu, Weixin / Zhang, Yuhua | 2006
34
Novel 6,7,8,9-tetrahydro-5H-1,4,7,10a-tetraaza-cyclohepta[f]indene analogues as potent and selective 5-HT2C agonists for the treatment of metabolic disorders
Tye, Heather / Mueller, Stephan G. / Prestle, Juergen / Scheuerer, Stefan / Schindler, Marcus / Nosse, Bernd / Prevost, Natacha / Brown, Christopher J. / Heifetz, Alexander / Moeller, Clemens et al. | 2010
34
Design, synthesis, and evaluation of caffeic acid amides as synergists to sensitize fluconazole-resistant Candida albicans to fluconazole
Dai, Li / Zang, Chengxu / Tian, Shujuan / Liu, Wei / Tan, Shanlun / Cai, Zhan / Ni, Tingjunhong / An, Maomao / Li, Ran / Gao, Yue et al. | 2014
34
New polyhydroxytriterpenoid derivatives from fruits of Terminalia chebula Retz. and their α-glucosidase and α-amylase inhibitory activity
Lee, Dong Young / Yang, Heejung / Kim, Hyun Woo / Sung, Sang Hyun | 2016
35
A novel series of highly potent 5-lipoxygenase inhibitors; 2-aryldienylbenzoxazoles
Kosaka, T. / Ochiai, K. / Ohba, S. / Wakabayashi, T. / Murota, S. | 1995
35
A new class of diacidic nonpeptide angiotensin II receptor antagonists
Cho, N. / Kubo, K. / Furuya, S. / Sugiura, Y. / T., Yasuma / Y., Kohara / M., Ojima / Y., Inada / K., Nishikawa / T., Naka | 1993
35
Chemical and enzymatic synthesis of glycoconjugates. Part 5: One-pot regioselective synthesis of bioactive galactobiosides using a CLONEZYMETM thermophilic glycosidase library
Li, J. / Robertson, D.E. / Short, J.M. / Wang, P.G. | 1999
35
Synthesis of bis-spermine dimers that are potent polyamine transport inhibitors
Graminski, Gerard F. / Carlson, C.Lance / Ziemer, Josh R. / Cai, Feng / Vermeulen, Nicolaas M.J. / Vanderwerf, Scott M. / Burns, Mark R. | 2002
35
Pyrazole derived from (+)-3-carene; a novel potent, selective scaffold for sphingosine-1-phosphate (S1P1) receptor agonists
Zécri, Frédéric J. / Albert, Rainer / Landrum, Gregory / Hinterding, Klaus / Cooke, Nigel G. / Guerini, Danilo / Streiff, Markus / Bruns, Christian / Nuesslein-Hildesheim, Barbara | 2009
35
Synthesis and structure-activity relationships of 4-oxo-1-phenyl-3,4,6,7-tetrahydro-(1,4)diazepino(6,7,1-hi)indoles: novel PDE4 inhibitors
Pascal, Yves / Andrianjara, Charles R. / Auclair, Eric / Avenel, Nadine / Bertin, Bernadette / Calvet, Alain / Féru, Frédéric / Lardon, Sophie / Moodley, Indres / Ouagued, Malika et al. | 2000
35
Selective incorporation of foreign functionality into fibrin gels through a chemically modified DNA aptamer
Fujita, Hiroto / Inoue, Yusuke / Kuwahara, Masayasu | 2018
35
Sugar-substituted 2-azetidinones as cholesterol absorption inhibitors
Vaccaro, W.D. / Sher, R. / Jr, H.R.Davis | 1998
36
PEG-immobilization of cardol and soluble polymer-supported synthesis of some cardol–coumarin derivatives: Preliminary evaluation of their inhibitory activity on mushroom tyrosinase
Tocco, Graziella / Fais, Antonella / Meli, Gabriele / Begala, Michela / Podda, Gianni / Fadda, M.Benedetta / Corda, Marcella / Attanasi, Orazio A. / Filippone, Paolino / Berretta, Stefano | 2008
36
Peptide inhibitors of dengue virus NS3 protease. Part 1: Warhead
Yin, Zheng / Patel, Sejal J. / Wang, Wei-Ling / Wang, Gang / Chan, Wai-Ling / Rao, K.R. Ranga / Alam, Jenefer / Jeyaraj, Duraiswamy A. / Ngew, Xinyi / Patel, Viral et al. | 2005
36
Discovery of covalent enzyme inhibitors using virtual docking of covalent fragments
Chowdhury, Sandipan Roy / Kennedy, Steven / Zhu, Kai / Mishra, Rama / Chuong, Patrick / Nguyen, Alyssa-uyen / Kathman, Stefan G. / Statsyuk, Alexander V. | 2019
37
Synthesis and γ-secretase activity of APP substrate-based hydroxyethylene dipeptide isosteres
Nadin, Alan / Owens, Andrew P. / Castro, José L. / Harrison, Timothy / Shearman, Mark S. | 2002
37
Synthesis of RP-67,580, a new potent nonpeptide substance P antagonist
Peyronel, Jean-François / Truchon, Alain / Moutonnier, Claude / Garret, Claude | 1991
37
Anti-coxsackievirus B3 activity of 2-amino-3-nitropyrazolo[1,5-a]pyrimidines and their analogs
Makarov, Vadim A. / Riabova, Olga B. / Granik, Vladimir G. / Dahse, Hans-Martin / Stelzner, Axel / Wutzler, Peter / Schmidtke, Michaela | 2004
37
Development of an in vivo active, dual EP1 and EP3 selective antagonist based on a novel acyl sulfonamide bioisostere
Downey, Jason D. / Saleh, Sam A. / Bridges, Thomas M. / Morrison, Ryan D. / Scott Daniels, J. / Lindsley, Craig W. / Breyer, Richard M. | 2012
37
Structure-activity studies of CTL inhibitory peptides derived from HLA class I molecules
Schwartz, E.J. / Goldberg, J. / Clayberger, C. / Krensky, A.M. / Griffin, J.H. | 1997
37
Anthranilate 4H-oxazol-5-ones: novel small molecule antibacterial acyl carrier protein synthase (AcpS) inhibitors
Gilbert, Adam M. / Kirisits, Matthew / Toy, Patrick / Nunn, David S. / Failli, Amadeo / Dushin, Elizabeth G. / Novikova, Elena / Petersen, Peter J. / Joseph-McCarthy, Diane / McFadyen, Iain et al. | 2003
37
Synthesis and g-secretase activity of APP substrate-based hydroxyethylene dipeptide isosteres
Nadin, Alan / Owens, Andrew P. / Castro, José L. / Harrison, Timothy / Shearman, Mark S. | 2003
38
Synthesis and biological evaluation of a novel artesunate–podophyllotoxin conjugate as anticancer agent
Zhang, Lei / Chen, Fan / Zhang, Zeguo / Chen, Yongzheng / Wang, Jing | 2015
38
3D QSAR studies on 3,4-dihydroquinazolines as T-type calcium channel blocker by comparative molecular similarity indices analysis (CoMSIA)
Jeong, Jin Ah / Cho, Haelim / Jung, Soo Yeon / Kang, Han Byul / Park, Jin Yeong / Kim, Jungahn / Choo, Dong Joon / Lee, Jae Yeol | 2009
38
Trishomocubane as a scaffold for the development of selective dopamine transporter (DAT) ligands
Banister, Samuel D. / Moussa, Iman A. / Beinat, Corinne / Reynolds, Aaron J. / Schiavini, Paolo / Jorgensen, William T. / Kassiou, Michael | 2010
38
Synthesis and characterization of monodisperse poly(ethylene glycol)-conjugated collagen pentapeptides with collagen biosynthesis-stimulating activity
Kim, Myung Sun / Park, Eun Ji / Na, Dong Hee | 2014
39
Synthesis and biological activity of piperazine and diazepane amides that are histamine H3 antagonists and serotonin reuptake inhibitors
Ly, Kiev S. / Letavic, Michael A. / Keith, John M. / Miller, Jennifer M. / Stocking, Emily M. / Barbier, Ann J. / Bonaventure, Pascal / Lord, Brian / Jiang, Xiaohui / Boggs, Jamin D. et al. | 2007
39
Design, synthesis, and activity evaluation of broad-spectrum small-molecule inhibitors of anti-apoptotic Bcl-2 family proteins: Characteristics of broad-spectrum protein binding and its effects on anti-tumor activity
Zheng, Can-Hui / Yang, Hui / Zhang, Meng / Lu, Shi-Hai / Shi, Duo / Wang, Juan / Chen, Xiu-Hua / Ren, Xiao-Hui / Liu, Jia / Lv, Jia-Guo et al. | 2011
39
Design and synthesis of Rhodamine 110 derivative and Caspase-3 substrate for enzyme and cell-based fluorescent assay
Cai, Sui Xiong / Zhang, Han-Zhong / Guastella, John / Drewe, John / Yang, Wu / Weber, Eckard | 2001
39
Synthesis and anticonvulsant activity of the (+)- and (-)-enantiomers of 1,2,3,4-tetrahydro-5-(2-phosphonoethyl)-3-isoqulnolinecarboxylic acid, a competitive NMDA antagonist
Biqge, C.F. / Wu, J.-P. / Malone, T.C. / Taylor, C.P. / Vartanian, M.G. | 1993
39
Design and synthesis of highly potent fumagillin analogues from homology modeling for a human MetAP-2
Han, Cheol Kyu / Ahn, Soon Kil / Choi, Nam Song / Hong, Ryung Kee / Moon, Seung Kee / Chun, Hyoung Sik / Lee, Sang Joon / Kim, Jung Woo / Hong, Chung Il / Kim, Deukjoon et al. | 2000
39
A facile synthesis of 2-azidoadenosine derivatives from guanosine as photoaffinity probes
Higashiya, S. / Kaibara, C. / Fukuoka, K. / Suda, F. / Ishikawa, M. / Yoshida, M. / Hata, T. | 1996
39
The synthesis and dopamine D2 and serotonin 5-HT3 receptor affinity of 3-aza analogues (pyridyl) of 4-amino-5-chloro-2-methoxybenzamides
Coldwell, M.C. / Gadre, A. / Jerman, J. / King, F.D. / Nash, D. | 1995
39
Design and synthesis of 6-(6-D-ribitylamino-2, 4-dihydroxypyrimidin-5-yl)-1- hexylphosphonic acid, a potent inhibitor of lumazine synthase
Cushman, M. / Mihalic, J.T. / Kis, K. / Bacher, A. | 1999
39
Synthesis and anticonvulsant activity of the (+)- and (−)-enantiomers of 1,2,3,4-tetrahydro-5-(2-phosphonoethyl)-3-isoquinolinecarboxylic acid, a competitive NMDA antagonist
Bigge, Christopher F. / Wu, Jiang-Ping / Malone, Thomas C. / Taylor, Charles P. / Vartanian, Mark G. | 1993
40
Design, synthesis and anti-Alzheimer properties of dimethylaminomethyl-substituted curcumin derivatives
Fang, Lei / Gou, Shaohua / Liu, Xuying / Cao, Feng / Cheng, Lin | 2013
40
Identification and synthesis of 2,7-diamino-thiazolo[5,4-d]pyrimidine derivatives as TRPV1 antagonists
Lebsack, Alec D. / Branstetter, Bryan J. / Hack, Michael D. / Xiao, Wei / Peterson, Matthew L. / Nasser, Nadia / Maher, Michael P. / Ao, Hong / Bhattacharya, Anindya / Kansagara, Mena et al. | 2008
40
Parallel strategies for the preparation and selection of liver-targeted glucocorticoid receptor antagonists
Backes, Bradley J. / Hamilton, Gregory L. / Nguyen, Phong / Wilcox, Denise / Fung, Steven / Wang, Jiahong / Grynfarb, Marlena / Goos-Nilsson, Annika / Jacobson, Peer B. / von Geldern, Thomas W. | 2006
40
Peptide inhibitors of dengue virus NS3 protease. Part 2: SAR study of tetrapeptide aldehyde inhibitors
Yin, Zheng / Patel, Sejal J. / Wang, Wei-Ling / Chan, Wai-Ling / Ranga Rao, K.R. / Wang, Gang / Ngew, Xinyi / Patel, Viral / Beer, David / Knox, John E. et al. | 2005
40
Anthraquinones from Morinda longissima and their insulin mimetic activities via AMP-activated protein kinase (AMPK) activation
Nguyen, Phi-Hung / Choi, Hong Seok / Ha, Thi Kim Quy / Seo, Ji Yeon / Yang, Jun-Li / Jung, Da-Woon / Williams, Darren R. / Oh, Won-Keun | 2016
40
Antiplasmodial alkaloids from bulbs of Amaryllis belladonna Steud.
Cho, Namki / Du, Yongle / Valenciano, Ana Lisa / Fernández-Murga, Maria L. / Goetz, Michael / Clement, Jason / Cassera, Maria B. / Kingston, David G.I. | 2018
40
Novel monoamine oxidase inhibitors based on the privileged 2-imidazoline molecular framework
Shetnev, Anton / Osipyan, Angelina / Baykov, Sergey / Sapegin, Alexander / Chirkova, Zhanna / Korsakov, Michail / Petzer, Anél / Engelbrecht, Idalet / Petzer, Jacobus P. | 2019
41
Identified a morpholinyl-4-piperidinylacetic acid derivative as a potent oral active VLA-4 antagonist
Chiba, Jun / Machinaga, Nobuo / Takashi, Tohru / Ejima, Akio / Takayama, Gensuke / Yokoyama, Mika / Nakayama, Atsushi / Baldwin, John J. / McDonald, Edward / Saionz, Kurt W. et al. | 2004
41
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Kim, Dooseop / Mantlo, Nathan B. / Chang, R.S.L. / Kivlighn, S.D. / Greenlee, W.J. | 1993
41
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Cho, W.-J. / Park, M.-J. / Chung, B.-H. / Lee, C.-O. | 1998
41
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Graybill, T. L. / Prouty, C. P. / Speier, G. J. / Hoyer, D. / Dolle, R. E. / Helaszek, C. T. / Ator, M. A. / Uhl, J. / Strasters, J. | 1997
41
Thrombin active site inhibitors: chemical synthesis, in vitro and in vivo pharmacological profile of a novel and selective agent BMS-189090 and analogues
Das, Jagabandhu / Kimball, S.David / Reid, Joyce A. / Wang, Tammy C. / Lau, Wan F. / Roberts, Daniel G.M. / Seiler, Steven M. / Schumacher, William A. / Ogletree, Martin L. | 2002
41
a-((Tetronoyl)oxy)- and a-((tetramoyl)oxy)methyl ketone inhibitors of the interleukin-1b converting enzyme (ICE)
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41
An enzymatic synthesis of 2-azido-L-tyrosine
Hebel, D. / Furlano, D.C. / Phillips, R.S. / Koushik, S. / Creveling, C.R. / Kirk, K.L. | 1991
42
Synthesis and insecticidal evaluation of novel N-pyridylpyrazolecarboxamides containing cyano substituent in the ortho-position
Mao, Mingzhen / Li, Yuxin / Liu, Qiaoxia / Zhou, Yunyun / Zhang, Xiulan / Xiong, Lixia / Li, Yongqiang / Li, Zhengming | 2012
42
Novel tetrahydropyrido[3,2-c]pyrroles as 5-HT7 antagonists
Rudolph, Dale A. / Dvorak, Curt A. / Dvorak, Lisa / Nepomuceno, Diane / Bonaventure, Pascal / Lovenberg, Timothy W. / Carruthers, Nicholas I. | 2010
42
2,6-Dithienyl-4-furyl pyridines: Synthesis, topoisomerase I and II inhibition, cytotoxicity, structure–activity relationship, and docking study
Basnet, Arjun / Thapa, Pritam / Karki, Radha / Choi, Hoyoung / Choi, Jae Hun / Yun, Minho / Jeong, Byeong-Seon / Jahng, Yurngdong / Na, Younghwa / Cho, Won-Jea et al. | 2009
43
4-Amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors
Parmee, Emma R. / He, Jiafang / Mastracchio, Anthony / Edmondson, Scott D. / Colwell, Larry / Eiermann, George / Feeney, William P. / Habulihaz, Bahanu / He, Huaibing / Kilburn, Ruth et al. | 2003
43
Homologues and isomers of noladin ether, a putative novel endocannabinoid: interaction with rat cannabinoid CB1 receptors
Appendino, Giovanni / Ligresti, Alessia / Minassi, Alberto / Daddario, Nives / Bisogno, Tiziana / Di Marzo, Vincenzo | 2002
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