Discovery of novel pyrrolidineoxy-substituted heteroaromatics as potent and selective PI3K delta inhibitors with improved physicochemical properties (English)
- New search for: Hoegenauer, K.
- New search for: Soldermann, N.
- New search for: Hebach, C.
- New search for: Hollingworth, G. J.
- New search for: Lewis, I.
- New search for: von Matt, A.
- New search for: Smith, A. B.
- New search for: Wolf, R. M.
- New search for: Wilcken, R.
- New search for: Haasen, D.
- New search for: Hoegenauer, K.
- New search for: Soldermann, N.
- New search for: Hebach, C.
- New search for: Hollingworth, G. J.
- New search for: Lewis, I.
- New search for: von Matt, A.
- New search for: Smith, A. B.
- New search for: Wolf, R. M.
- New search for: Wilcken, R.
- New search for: Haasen, D.
In:
BIOORGANIC AND MEDICINAL CHEMISTRY LETTERS ONLINE
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26
, 23
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5657-5662
;
2016
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ISSN:
- Article (Journal) / Print
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Title:Discovery of novel pyrrolidineoxy-substituted heteroaromatics as potent and selective PI3K delta inhibitors with improved physicochemical properties
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Contributors:Hoegenauer, K. ( author ) / Soldermann, N. ( author ) / Hebach, C. ( author ) / Hollingworth, G. J. ( author ) / Lewis, I. ( author ) / von Matt, A. ( author ) / Smith, A. B. ( author ) / Wolf, R. M. ( author ) / Wilcken, R. ( author ) / Haasen, D. ( author )
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Published in:BIOORGANIC AND MEDICINAL CHEMISTRY LETTERS ONLINE ; 26, 23 ; 5657-5662
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Publisher:
- New search for: Elsevier Science B.V., Amsterdam.
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Publication date:2016-01-01
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Size:6 pages
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ISSN:
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Type of media:Article (Journal)
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Type of material:Print
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Language:English
- New search for: 572.5
- Further information on Dewey Decimal Classification
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Classification:
DDC: 572.5 -
Source:
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Table of contents – Volume 26, Issue 23
The tables of contents are generated automatically and are based on the data records of the individual contributions available in the index of the TIB portal. The display of the Tables of Contents may therefore be incomplete.
- 5603
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GPR40 agonists for the treatment of type 2 diabetes mellitus: The biological characteristics and the chemical spaceChen, Cheng / Li, He / Long, Ya-Qiu et al. | 2016
- 5613
-
Novel 5-substituted 3-hydroxyphenyl and 3-nitrophenyl ethers of S-prolinol as α4β2-nicotinic acetylcholine receptor ligandsBolchi, Cristiano / Bavo, Francesco / Fumagalli, Laura / Gotti, Cecilia / Fasoli, Francesca / Moretti, Milena / Pallavicini, Marco et al. | 2016
- 5618
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ProTides of BVdU as potential anticancer agents upon efficient intracellular delivery of their activated metabolitesKandil, Sahar / Balzarini, Jan / Rat, Stephanie / Brancale, Andrea / Westwell, Andrew D. / McGuigan, Christopher et al. | 2016
- 5624
-
Multiple biological activities and molecular docking studies of newly synthesized 3-(pyridin-4-yl)-1H-pyrazole-5-carboxamide chalcone hybridsSribalan, Rajendran / Banuppriya, Govindharasu / Kirubavathi, Maruthan / Jayachitra, A. / Padmini, Vediappen et al. | 2016
- 5631
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3D-QSAR studies of 3-(3,4-dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic acids as AKR1C3 inhibitors: Highlight the importance of molecular docking in conformation generationZheng, Xuehua / Wu, Yinuo / Wu, Deyan / Wang, Xinhua / Zhang, Chao / Guo, Xiaolei / Luo, Hai-Bin et al. | 2016
- 5639
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The comparison of neuroprotective effects of isoliquiritigenin and its Phase I metabolites against glutamate-induced HT22 cell deathYang, Eun-Ju / Kim, Minjun / Woo, Ji Eun / Lee, Taeho / Jung, Jong-Wha / Song, Kyung-Sik et al. | 2016
- 5644
-
Gating role of His 72 in TmPurL enzyme uncovered by structural analyses and molecular dynamics simulationsGhosh, Biplab / Goyal, Venuka Durani et al. | 2016
- 5650
-
Synthesis and biological assessment of novel N-(hydroxy/methoxy)alkyl β-enaminone curcuminoidsTheppawong, Atiruj / De Vreese, Rob / Vannecke, Lore / Grootaert, Charlotte / Van Camp, John / D’hooghe, Matthias et al. | 2016
- 5657
-
Discovery of novel pyrrolidineoxy-substituted heteroaromatics as potent and selective PI3K delta inhibitors with improved physicochemical propertiesHoegenauer, Klemens / Soldermann, Nicolas / Hebach, Christina / Hollingworth, Gregory J. / Lewis, Ian / von Matt, Anette / Smith, Alexander B. / Wolf, Romain M. / Wilcken, Rainer / Haasen, Dorothea et al. | 2016
- 5663
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Novel bicyclo[3.1.0]hexane analogs as antagonists of metabotropic glutamate 2/3 receptors for the treatment of depressionDressman, Bruce A. / Tromiczak, Eric G. / Chappell, Mark D. / Tripp, Allie E. / Quimby, Steven J. / Vetman, Tatiana / Fivush, Adam M. / Matt, James / Jaramillo, Carlos / Li, Renhua et al. | 2016
- 5669
-
Identification of lead small molecule inhibitors of glycogen synthase kinase-3 beta using a fragment-linking strategyKim, Jinhee / Moon, Yonghoon / Hong, Sungwoo et al. | 2016
- 5674
-
Synthesis and biological evaluation of heteroaryl styryl sulfone derivatives as anticancer agentsLong, Yi / Yu, Mingfeng / Li, Peng / Islam, Saiful / Goh, Aik Wye / Kumarasiri, Malika / Wang, Shudong et al. | 2016
- 5679
-
Discovery of 4-chloro-3-(5-(pyridin-3-yl)-1,2,4-oxadiazole-3-yl)benzamides as novel RET kinase inhibitorsHan, Mei / Li, Shan / Ai, Jing / Sheng, Rong / Hu, Yongzhou / Hu, Youhong / Geng, Meiyu et al. | 2016
- 5685
-
Trityl radicals in perfluorocarbon emulsions as stable, sensitive, and biocompatible oximetry probesDhimitruka, Ilirian / Alzarie, Yasmin Alsayed / Hemann, Craig / Samouilov, Alexandre / Zweier, Jay L. et al. | 2016
- 5689
-
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examplesMcLeod, Michael C. / Aubé, Jeffrey / Frankowski, Kevin J. et al. | 2016
- 5695
-
Discovery of a potent and selective ROMK inhibitor with improved pharmacokinetic properties based on an octahydropyrazino[2,1-c][1,4]oxazine scaffoldZhu, Yuping / de Jesus, Reynalda K. / Tang, Haifeng / Walsh, Shawn P. / Jiang, Jinlong / Gu, Xin / Teumelsan, Nardos / Shahripour, Aurash / Pio, Barbara / Ding, Fa-Xiang et al. | 2016
- 5703
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Novel synthetic chalcones induce apoptosis in the A549 non-small cell lung cancer cells harboring a KRAS mutationWang, Yiqiang / Hedblom, Andreas / Koerner, Steffi K. / Li, Mailin / Jernigan, Finith E. / Wegiel, Barbara / Sun, Lijun et al. | 2016
- 5707
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[2.2.1]-Bicyclic sultams as potent androgen receptor antagonistsShan, Weifang / Balog, Aaron / Nation, Andrew / Zhu, Xiao / Chen, Jing / Cvijic, Mary Ellen / Geng, Jieping / Rizzo, Cheryl A. / Spires, Thomas Jr. / Attar, Ricardo M. et al. | 2016
- 5712
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First molecular modeling report on novel arylpyrimidine kynurenine monooxygenase inhibitors through multi-QSAR analysis against Huntington’s disease: A proposal to chemists!Amin, Sk. Abdul / Adhikari, Nilanjan / Jha, Tarun / Gayen, Shovanlal et al. | 2016
- 5719
-
Synthesis and biological evaluation of novel 2,4,5-triarylimidazole–1,2,3-triazole derivatives via click chemistry as α-glucosidase inhibitorsWang, Guangcheng / Peng, Zhiyun / Wang, Jing / Li, Juan / Li, Xin et al. | 2016
- 5724
-
Discovery of benzofuran propanoic acid GPR120 agonists: From uHTS hit to mechanism-based pharmacodynamic effectsLombardo, Matthew / Bender, Kate / London, Clare / Kirkland, Melissa / Mane, Joel / Pachanski, Michele / Geissler, Wayne / Cummings, John / Habulihaz, Bahanu / Akiyama, Taro E. et al. | 2016
- 5729
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Discovery of furo[2,3-d][1,3]thiazinamines as beta amyloid cleaving enzyme-1 (BACE1) inhibitorsWu, Yong-Jin / Guernon, Jason / Rajamani, Ramkumar / Toyn, Jeremy H. / Ahlijanian, Michael K. / Albright, Charles F. / Muckelbauer, Jodi / Chang, ChiehYing / Camac, Dan / Macor, John E. et al. | 2016
- 5732
-
Gastroprotective activity of synthetic coumarins: Role of endogenous prostaglandins, nitric oxide, non-protein sulfhydryls and vanilloid receptorsSepulveda, Beatriz / Quispe, Cristina / Simirgiotis, Mario / Torres-Benítez, Alfredo / Reyes-Ortíz, Johanna / Areche, Carlos / García-Beltrán, Olimpo et al. | 2016
- 5736
-
Novel fluorescent substrates for detection of trypsin activity and inhibitor screening by self-quenchingSato, Daisuke / Kato, Tamaki et al. | 2016
- 5741
-
Discovery of indazole ethers as novel, potent, non-steroidal glucocorticoid receptor modulatorsHemmerling, Martin / Edman, Karl / Lepistö, Matti / Eriksson, Anders / Ivanova, Svetlana / Dahmén, Jan / Rehwinkel, Hartmut / Berger, Markus / Hendrickx, Ramon / Dearman, Matthew et al. | 2016
- 5749
-
Design, synthesis, antibacterial activity and docking study of some new trimethoprim derivativesRashid, Umer / Ahmad, Waqas / Hassan, Syed Fahad / Qureshi, Naveeda Akhtar / Niaz, Basit / Muhammad, Bakhtiar / Imdad, Sameera / Sajid, Muhammad et al. | 2016
- 5754
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Thioxylated cyclosporin A for studying protein–drug interactionsLin, Weilin / Erdmann, Frank / Quintero, Andres / Fischer, Gunter / Zhang, Yixin et al. | 2016
- 5757
-
Discovery, characterization and biological evaluation of a novel (R)-4,4-difluoropiperidine scaffold as dopamine receptor 4 (D4R) antagonistsJeffries, Daniel E. / Witt, Jonathan O. / McCollum, Andrea L. / Temple, Kayla J. / Hurtado, Miguel A. / Harp, Joel M. / Blobaum, Anna L. / Lindsley, Craig W. / Hopkins, Corey R. et al. | 2016
- 5765
-
Functional 1,3a,6a-triazapentalene scaffold: Design of fluorescent probes for kinesin spindle protein (KSP)Sawada, Jun-ichi / Osawa, Ayumi / Takeuchi, Tomoki / Kaneda, Masato / Oishi, Shinya / Fujii, Nobutaka / Asai, Akira / Tanino, Keiji / Namba, Kosuke et al. | 2016
- 5770
-
Design and synthesis of the penta(acetoxymethyl) ester of dioctanoyl phosphatidylinositol-3,5-bisphosphateKanoh, Naoki / Mano, Kosuke / Saigusa, Daisuke / Usui, Takeo / Iwabuchi, Yoshiharu et al. | 2016
- 5773
-
Cytotoxic lanostanes from fruits of Garcinia wallichii Choisy (Guttiferae)Hongthong, Sakchai / Meesin, Jatuporn / Pailee, Phanruethai / Soorukram, Darunee / Kongsaeree, Palangpon / Prabpai, Samran / Piyachaturawat, Pawinee / Jariyawat, Surawat / Suksen, Kanoknetr / Jaipetch, Thaworn et al. | 2016
- 5780
-
Discovery of a potent and highly specific β2 proteasome inhibitor from a library of copper complexesZhou, Tongliang / Cai, Yuanbo / Liang, Lei / Yang, Lingfei / Xu, Fengrong / Niu, Yan / Wang, Chao / Zhang, Jun-Long / Xu, Ping et al. | 2016
- 5785
-
68Ga labeled fatty acids for cardiac metabolic imaging: Influence of different bifunctional chelatorsJain, Akanksha / Mathur, Anupam / Pandey, Usha / Sarma, Haladhar Dev / Dash, Ashutosh et al. | 2016
- 5792
-
Development of pharmacophore models for small molecules targeting RNA: Application to the RNA repeat expansion in myotonic dystrophy type 1Angelbello, Alicia J. / González, Àlex L. / Rzuczek, Suzanne G. / Disney, Matthew D. et al. | 2016
- 5797
-
Chalcone–benzoxaborole hybrids as novel anticancer agentsZhang, Jiong / Yang, Fei / Qiao, Zhitao / Zhu, Mingyan / Zhou, Huchen et al. | 2016
- 5802
-
Discovery of phenoxyindazoles and phenylthioindazoles as RORγ inverse agonistsOuvry, Gilles / Bouix-Peter, Claire / Ciesielski, Fabrice / Chantalat, Laurent / Christin, Olivier / Comino, Catherine / Duvert, Denis / Feret, Christophe / Harris, Craig S. / Lamy, Laurent et al. | 2016
- 5809
-
Discovery of highly potent and selective orexin 1 receptor antagonists (1-SORAs) suitable for in vivo interrogation of orexin 1 receptor pharmacologyStump, Craig A. / Cooke, Andrew J. / Bruno, Joseph / Cabalu, Tamara D. / Gotter, Anthony L. / Harell, C. Meacham / Kuduk, Scott D. / McDonald, Terrence P. / O’Brien, Julie / Renger, John J. et al. | 2016
- 5815
-
Synthesis of novel Ral inhibitors: An in vitro and in vivo studyYan, Chao / Theodorescu, Dan / Miller, Bettina / Kumar, Amit / Kumar, Vijay / Ross, David / Wempe, Michael F. et al. | 2016
- 5819
-
Novel substituted aminothiazoles as potent and selective anti-hepatocellular carcinoma agentsLu, Huagang / Rogowskyj, John / Yu, Wenquan / Venkatesh, Anu / Khan, Noshena / Nakagawa, Shigeki / Goossens, Nicolas / Koh, Anna P. / Higashi, Takaaki / Gunasekaran, Ganesh et al. | 2016
- 5825
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Design, synthesis, and evaluation of (2S,4R)-Ketoconazole sulfonamide analogs as potential treatments for Metabolic SyndromeBlass, Benjamin E. / Iyer, Pravin / Abou-Gharbia, Magid / Childers, Wayne E. / Gordon, John C. / Ramanjulu, Mercy / Morton, George / Arumugam, Premkumar / Boruwa, Joshodeep / Ellingboe, John et al. | 2016
- 5830
-
Design, synthesis, and biological activity of 4-(imidazo[1,2-b]pyridazin-3-yl)-1H-pyrazol-1-yl-phenylbenzamide derivatives as BCR–ABL kinase inhibitorsHu, Liming / Cao, Tingting / Lv, Yongjuan / Ding, Yiming / Yang, Leifu / Zhang, Qiang / Guo, Mingzhou et al. | 2016
- 5836
-
Design and synthesis of water soluble β-aminosulfone analogues of SCH 900229 as γ-secretase inhibitorsWu, Wen-Lian / Burnett, Duane A. / Clader, John / Greenlee, William J. / Jiang, Qin / Hyde, Lynn A. / Del Vecchio, Robert A. / Cohen-Williams, Mary E. / Song, Lixin / Lee, Julie et al. | 2016
- IFC
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Editorial board| 2016