Challenges in the development of an M4 PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs (English)
- New search for: Wood, Michael R
- New search for: Wood, Michael R
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- New search for: Poslusney, Michael S
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- New search for: Lamsal, Atin
- New search for: Chang, Sichen
- New search for: Luscombe, Vincent B
- New search for: Weiner, Rebecca L
- New search for: Cho, Hyekyung P
- New search for: Bubser, Michael
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In:
Bioorganic & medicinal chemistry letters
;
27
, 2
; 171-175
;
2017
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ISSN:
- Article (Journal) / Print
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Title:Challenges in the development of an M4 PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs
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Contributors:
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Published in:Bioorganic & medicinal chemistry letters ; 27, 2 ; 171-175
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Publisher:
- New search for: Elsevier
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Place of publication:Amsterdam [u.a.]
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Publication date:2017
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ISSN:
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ZDBID:
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DOI:
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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: 35.70 / 44.33 / 44.42
- Further information on Basic classification
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Source:
Table of contents – Volume 27, Issue 2
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.
- 121
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Intelligent substance delivery into cells using cell-penetrating peptidesTashima, Toshihiko et al. | 2016
- 131
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Antiproliferative activity and SARs of caffeic acid esters with mono-substituted phenylethanols moietyXie, Jin / Yang, Fengzhi / Zhang, Man / Lam, Celine / Qiao, Yixue / Xiao, Jia / Zhang, Dongdong / Ge, Yuxuan / Fu, Lei / Xie, Dongsheng et al. | 2016
- 135
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Synthesis and antiproliferative activity of 2-chlorophenyl carboxamide thienopyridinesvan Rensburg, Michelle / Leung, Euphemia / Haverkate, Natalie A. / Eurtivong, Chatchakorn / Pilkington, Lisa I. / Reynisson, Jóhannes / Barker, David et al. | 2016
- 139
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Synthesis and in vitro antiviral evaluation of 4-substituted 3,4-dihydropyrimidinonesKumarasamy, Dhanabal / Roy, Biswajit Gopal / Rocha-Pereira, Joana / Neyts, Johan / Nanjappan, Satheeshkumar / Maity, Subhasis / Mookerjee, Musfiqua / Naesens, Lieve et al. | 2016
- 143
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Imidazopyridyl compounds as aldosterone synthase inhibitorsWhitehead, Brent R. / Lo, Michael M.-C. / Ali, Amjad / Park, Min K. / Hoyt, Scott B. / Xiong, Yusheng / Cai, Jiaqiang / Carswell, Emma / Cooke, Andrew / MacLean, John et al. | 2016
- 147
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Design, synthesis and cytotoxic activities of scopoletin-isoxazole and scopoletin-pyrazole hybridsShi, Wei / Hu, Jinglin / Bao, Na / Li, Dongang / Chen, Li / Sun, Jianbo et al. | 2016
- 152
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Synthesis and biological properties of galactofuranosyl-containing fluorescent dyesLegentil, Laurent / Belaz, Sorya / Gangneux, Jean-Pierre / Robert-Gangneux, Florence / Ferrières, Vincent et al. | 2016
- 156
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Photodynamic effect of meso-(aryl)porphyrins and meso-(1-methyl-4-pyridinium)porphyrins on HaCaT keratinocytesSlomp, Amanda M. / Barreira, Sandra M.W. / Carrenho, Luise Z.B. / Vandresen, Camila C. / Zattoni, Ingrid F. / Ló, Stephanie M.S. / Dallagnol, Juliana C.C. / Ducatti, Diogo R.B. / Orsato, Alexandre / Duarte, M. Eugênia R. et al. | 2016
- 162
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Identification and validation of small molecule modulators of the NusB-NusE interactionCossar, Peter J. / Ma, Cong / Gordon, Christopher P. / Ambrus, Joseph I. / Lewis, Peter J. / McCluskey, Adam et al. | 2016
- 168
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Presence of negative supercoiling in aggregates of histone H1-plasmidic polynucleosome complexesZhang, Hao / Li, Tianhu et al. | 2016
- 171
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Challenges in the development of an M4 PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogsWood, Michael R. / Noetzel, Meredith J. / Poslusney, Michael S. / Melancon, Bruce J. / Tarr, James C. / Lamsal, Atin / Chang, Sichen / Luscombe, Vincent B. / Weiner, Rebecca L. / Cho, Hyekyung P. et al. | 2016
- 176
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In vivo and in silico anti-inflammatory mechanism of action of the semisynthetic (−)-cubebin derivatives (−)-hinokinin and (−)-O-benzylcubebinLima, Thaís C. / Lucarini, Rodrigo / Volpe, Angelica C. / de Andrade, Carolina Q.J. / Souza, Alice M.P. / Pauletti, Patricia M. / Januário, Ana H. / Símaro, Guilherme V. / Bastos, Jairo K. / Cunha, Wilson R. et al. | 2016
- 180
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Bivalent SIRT1 inhibitorsWang, Juan / Zang, Wenwen / Liu, Jiajia / Zheng, Weiping et al. | 2016
- 187
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Novel pyrazolo[1,5-a]pyridines with improved aqueous solubility as p110α-selective PI3 kinase inhibitorsKendall, Jackie D. / Giddens, Anna C. / Tsang, Kit Yee / Marshall, Elaine S. / Lill, Claire L. / Lee, Woo-Jeong / Kolekar, Sharada / Chao, Mindy / Malik, Alisha / Yu, Shuqiao et al. | 2016
- 191
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Synthesis and evaluation of the anti-proliferative activity of diaryl-3-pyrrolin-2-ones and fused analogsMowery, Patricia / Banales Mejia, Fernando / Franceschi, Courtney L. / Kean, Maeve H. / Kwansare, Deborah O. / Lafferty, Megan M. / Neerukonda, Namita D. / Rolph, Carly E. / Truax, Nathanyal J. / Pelkey, Erin T. et al. | 2016
- 196
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Synthesis, characterization, and in vitro SAR evaluation of N,N′-bis(arylmethyl)-C2-alkyl substituted imidazolium saltsDeBord, Michael A. / Wagers, Patrick O. / Crabtree, Steven R. / Tessier, Claire A. / Panzner, Matthew J. / Youngs, Wiley J. et al. | 2016
- 203
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Quinolizinium as a new fluorescent lysosomotropic probeZacharioudakis, Emmanouil / Cañeque, Tatiana / Custodio, Raúl / Müller, Sebastian / Cuadro, Ana M. / Vaquero, Juan J. / Rodriguez, Raphaël et al. | 2016
- 208
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Synthesis of 2-methyl-1,4-naphthoquinones with higher gamma-glutamyl carboxylase activity than MK-4 both in vitro and in vivoVermeer, Cees / van 't Hoofd, Cynthia / Knapen, Marjo H.J. / Xanthoulea, Sofia et al. | 2016
- 212
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Computational approach for the assessment of inhibitory potency against beta-amyloid aggregationBajda, Marek / Filipek, Sławomir et al. | 2016
- 217
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Novel 3-methylindoline inhibitors of EZH2: Design, synthesis and SARAnsari, Amantullah / Satalkar, Sharad / Patil, Varshavekumar / Shete, Amit S. / Kaur, Simranjeet / Gupta, Ashu / Singh, Siddhartha / Raja, Mohd. / Severance, Daniel L. / Bernales, Sebastián et al. | 2016
- 223
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Antimycobacterial activity of novel hydrazide-hydrazone derivatives with 2H-chromene and coumarin scaffoldAngelova, Violina T. / Valcheva, Violeta / Vassilev, Nikolay G. / Buyukliev, Rosen / Momekov, Georgi / Dimitrov, Ivan / Saso, Luciano / Djukic, Mirjana / Shivachev, Boris et al. | 2016
- 228
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Design and synthesis of new piperidone grafted acetylcholinesterase inhibitorsBasiri, Alireza / Xiao, Michelle / McCarthy, Alec / Dutta, Debashis / Byrareddy, Siddappa N. / Conda-Sheridan, Martin et al. | 2016
- 232
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Synthesis and application of β-carbolines as novel multi-functional anti-Alzheimer’s disease agentsHorton, William / Sood, Abha / Peerannawar, Swarada / Kugyela, Nandor / Kulkarni, Aditya / Tulsan, Rekha / Tran, Chris D. / Soule, Jessica / LeVine, Harry III / Török, Béla et al. | 2016
- 237
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Synthesis and in vitro antiproliferative activity of C5-benzyl substituted 2-amino-pyrrolo[2,3-d]pyrimidines as potent Hsp90 inhibitorsLee, Ju-Hyeon / Shin, Sang Chul / Seo, Seon Hee / Seo, Young Ho / Jeong, Nakcheol / Kim, Chan-Wha / Kim, Eunice EunKyeong / Keum, Gyochang et al. | 2016
- 242
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NMR strategies to support medicinal chemistry workflows for primary structure determinationOguadinma, Paul / Bilodeau, Francois / LaPlante, Steven R. et al. | 2016
- 248
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Biotransformation of isofraxetin-6-O-β-d-glucopyranoside by Angelica sinensis (Oliv.) Diels callusZhou, Di / Zhang, Yuhua / Jiang, Zhe / Hou, Yue / Jiao, Kun / Yan, Chunyan / Li, Ning et al. | 2016
- 254
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Fluorescent diphenylphosphonate-based probes for detection of serine protease activity during inflammationEdgington-Mitchell, Laura E. / Barlow, Nicholas / Aurelio, Luigi / Samha, Aminath / Szabo, Monika / Graham, Bim / Bunnett, Nigel et al. | 2016
- 261
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Novel carbazole sulfonamide derivatives of antitumor agent: Synthesis, antiproliferative activity and aqueous solubilitySun, Lianqi / Wu, Yanbin / Liu, Yonghua / Chen, Xiaofang / Hu, Laixing et al. | 2016
- 266
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Phytochemical and cytotoxic studies on the roots of Euphorbia fischerianaShi, Qun / Sun, Yi-wei / Meng, Dali et al. | 2016
- 271
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Design, synthesis and fungicidal activity of novel 2-substituted aminocycloalkylsulfonamidesLiu, Caixiu / Yan, Xiaojing / Wang, Minlong / Qin, Peiwen / Qi, Zhiqiu / Ji, Mingshan / Liu, Xingyu / Babu, P. Vijaya / Li, Xinghai / Cui, Zi-Ning et al. | 2016
- 277
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Virtual screening and biophysical studies lead to HSP90 inhibitorsHuang, Renjie / Ayine-Tora, Daniel M. / Muhammad Rosdi, M. Nasri / Li, Yu / Reynisson, Jóhannes / Leung, Ivanhoe K.H. et al. | 2016
- 282
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Squarate-based carbocyclic nucleosides: Syntheses, computational analyses and anticancer/antiviral evaluationLu, Meijun / Lu, Qing-Bin / Honek, John F. et al. | 2016
- 288
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New bithiazolyl hydrazones: Novel synthesis, characterization and antitubercular evaluationBhalerao, Mahendra B. / Dhumal, Sambhaji T. / Deshmukh, Amarsinh R. / Nawale, Laxman U. / Khedkar, Vijay / Sarkar, Dhiman / Mane, Ramrao A. et al. | 2016
- 295
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Discovery and initial optimization of alkoxyanthranilic acid derivatives as inhibitors of HCV NS5B polymeraseParcella, Kyle / Nickel, Andrew / Beno, Brett R. / Sheriff, Steven / Wan, Changhong / Wang, Ying-Kai / Roberts, Susan B. / Meanwell, Nicholas A. / Kadow, John F. et al. | 2016
- 299
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Synthesis of novel substituted pyrimidine derivatives bearing a sulfamide group and their in vitro cancer growth inhibition activityLefebvre, Carole-Anne / Forcellini, Elsa / Boutin, Sophie / Côté, Marie-France / C.-Gaudreault, René / Mathieu, Patrick / Lagüe, Patrick / Paquin, Jean-François et al. | 2016
- 303
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Structure-activity and in vivo evaluation of a novel lipoprotein lipase (LPL) activatorGeldenhuys, Werner J. / Caporoso, Joel / Leeper, Thomas C. / Lee, Yoon-Kwang / Lin, Li / Darvesh, Altaf S. / Sadana, Prabodh et al. | 2016
- 309
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Bioactive chemical constituents from the root bark of Morus australisLiao, Yu-Ren / Kuo, Ping-Chung / Tsai, Wei-Jern / Huang, Guan-Jhong / Lee, Kuo-Hsiung / Wu, Tian-Shung et al. | 2016
- 314
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Discovery of a new isomannide-based peptidomimetic synthetized by Ugi multicomponent reaction as human tissue kallikrein 1 inhibitorBarros, Thalita G. / Santos, Jorge A.N. / de Souza, Bruno E.G. / Sodero, Ana Carolina R. / de Souza, Alessandra M.T. / da Silva, Dayane P. / Rodrigues, Carlos Rangel / Pinheiro, Sergio / Dias, Luiza R.S. / Abrahim-Vieira, Bárbara et al. | 2016
- 319
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Development of a simple proton nuclear magnetic resonance-based procedure to estimate the approximate distribution coefficient at physiological pH (logD7.4): Evaluation and comparison to existing practicesStéen, E. Johanna L. / Nyberg, Nils / Lehel, Szabolcs / Andersen, Valdemar L. / Di Pilato, Pantaleo / Knudsen, Gitte M. / Kristensen, Jesper L. / Herth, Matthias M. et al. | 2016
- 323
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Discovery of dual positive allosteric modulators (PAMs) of the metabotropic glutamate 2 receptor and CysLT1 antagonists for treating migraine headacheBlanco, Maria-Jesus / Benesh, Dana R. / Knobelsdorf, James A. / Khilevich, Albert / Cortez, Guillermo S. / Mokube, Fese / Aicher, Thomas D. / Groendyke, Todd M. / Marmsater, Fredrik P. / Tang, Tony P. et al. | 2016
- 329
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Cyclic ferrocenylnaphthalene diimide derivative as a new class of G-quadruplex DNA binding ligandIslam, Md. Monirul / Sato, Shinobu / Shinozaki, Shingo / Takenaka, Shigeori et al. | 2016
- 336
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Affibody-displaying bio-nanocapsules effective in EGFR, typical biomarker, expressed in various cancer cellsNishimura, Yuya / Ezawa, Ryosuke / Ishii, Jun / Ogino, Chiaki / Kondo, Akihiko et al. | 2016
- 342
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Discovery of novel DNA methyltransferase 3A inhibitors via structure-based virtual screening and biological assaysShao, Zhiyuan / Xu, Pan / Xu, Wen / Li, Linjuan / Liu, Shien / Zhang, Rukang / Liu, Yu-Chih / Zhang, Chenhua / Chen, Shijie / Luo, Cheng et al. | 2016
- 347
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Synthesis of novel steroidal agonists, partial agonists, and antagonists for the glucocorticoid receptorJin, Zhuang / Lin, Hua / Srinivasan, Sathish / Nwachukwu, Jerome C. / Bruno, Nelson / Griffin, Patrick R. / Nettles, Kendall W. / Kamenecka, Theodore M. et al. | 2016
- 354
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Novel benzothiazine-piperazine derivatives by peptide-coupling as potential anti-proliferative agentsVenkatesh, Ramineni / Kasaboina, Suresh / Bidayat, Deepthi / Nikhil Kumar, U / Jain, Nishant / Tangeda, Saritha Jostna / Bantu, Rajashaker / Janardhan, Sridhara / Nagarapu, Lingaiah et al. | 2016
- IFC
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Editorial board| 2016