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Dive into the research topics where Jianping Cai is active.

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Featured researches published by Jianping Cai.


Bioconjugate Chemistry | 2015

DNA Compatible Multistep Synthesis and Applications to DNA Encoded Libraries

Alexander Lee Satz; Jianping Cai; Yi Chen; Robert Alan Goodnow; Felix Gruber; Agnieszka Kowalczyk; Ann Petersen; Goli Naderi-Oboodi; Lucja Orzechowski; Quentin Strebel

Complex mixtures of DNA encoded small molecules may be readily interrogated via high-throughput sequencing. These DNA encoded libraries (DELs) are commonly used to discover molecules that interact with pharmaceutically relevant proteins. The chemical diversity displayed by the library is key to successful discovery of potent, novel, and drug-like chemical matter. The small molecule moieties of DELs are generally synthesized though a multistep process, and each chemical step is accomplished while it is simultaneously attached to an encoding DNA oligomer. Hence, library chemical diversity is often limited to DNA compatible synthetic reactions. Herein, protocols for 24 reactions are provided that have been optimized for high-throughput production of DELs. These protocols detail the multistep synthesis of benzimidazoles, imidazolidinones, quinazolinones, isoindolinones, thiazoles, and imidazopyridines. Additionally, protocols are provided for a diverse range of useful chemical reactions including BOC deprotection (under pH neutral conditions), carbamylation, and Sonogashira coupling. Last, step-by-step protocols for synthesizing functionalized DELs from trichloronitropyrimidine and trichloropyrimidine scaffolds are detailed.


Bioorganic & Medicinal Chemistry Letters | 2012

Identification of novel, potent and selective inhibitors of Polo-like kinase 1.

Shaoqing Chen; David Joseph Bartkovitz; Jianping Cai; Yi Chen; Zhi Chen; Xin-Jie Chu; Kang Le; Nam T. Le; Kin-Chun Luk; Steve Mischke; Goli Naderi-Oboodi; John Frederick Boylan; Tom Nevins; Weiguo Qing; Yingsi Chen; Peter Michael Wovkulich

A series of pyrimidodiazepines was identified as potent Polo-like kinase 1 (PLK1) inhibitors. The synthesis and SAR are discussed. The lead compound 7 (RO3280) has potent inhibitory activity against PLK1, good selectivity against other kinases, and excellent in vitro cellular potency. It showed strong antitumor activity in xenograft mouse models.


Archive | 2008

Substituted pyrimidodiazepines useful as plk1 inhibitors

Jianping Cai; Shaoqing Chen; Xin-Jie Chu; Kang Le; Kin-Chun Luk; Peter Michael Wovkulich


Archive | 2003

Novel amino-substituted dihydropyrimido[4,5-d]pyrimidinone derivatives, their manufacture and use as pharmaceutical agents

Jianping Cai; Nikolaos Dimoudis; Konrad Honold; Kin-Chun Luk; Stefan Scheiblich; Hilke Sudergat; Georg Tiefenthaler; Oliver Tonn


Archive | 2009

HALO-SUBSTITUTED PYRIMIDODIAZEPINES AS PLKL INHIBITORS

Jianping Cai; Shaoqing Chen; Xin-Jie Chu; Kin-Chun Luk; Steven Gregory Mischke; Hongmao Sun; Peter Michael Wovkulich


Archive | 2004

Combinatorial library of 3-aryl-1h-indole-2-carboxylic acid

Jianping Cai; Robert Alan Goodnow


Archive | 2003

Amino-substituted dihydropyrimido[4,5-D]pyrimidinone derivatives

Jianping Cai; Nikolaos Dimoudis; Konrad Honold; Kin-Chun Luk; Stefan Scheiblich; Hilke Sudergat; Georg Tiefenthaler; Oliver Tonn


Archive | 2008

1- (indaz0l-5-yl) -ureas as diacylglycerol acyltransferase inhibitors

David Robert Bolin; Jianping Cai; Robert Alan Goodnow


Archive | 2007

4-phenyl-thiazole-5-carboxylic acids and 4-phenyl-thiazole-5-carboxylic acid amides as plk1 inhibitors

John Frederick Boylan; Jianping Cai; Nader Fotouhi; Paul Gillespie; Jr. Robert Alan Goodnow; Kang Le; Christophe Michoud


Archive | 2004

Solid phase synthesis of 3-aryl-2- indolylcarboxylic acids

Jianping Cai; Robert Alan Goodnow

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