Jianping Cai
Hoffmann-La Roche
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Publication
Featured researches published by Jianping Cai.
Bioconjugate Chemistry | 2015
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
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
Jianping Cai; Shaoqing Chen; Xin-Jie Chu; Kang Le; Kin-Chun Luk; Peter Michael Wovkulich
Archive | 2003
Jianping Cai; Nikolaos Dimoudis; Konrad Honold; Kin-Chun Luk; Stefan Scheiblich; Hilke Sudergat; Georg Tiefenthaler; Oliver Tonn
Archive | 2009
Jianping Cai; Shaoqing Chen; Xin-Jie Chu; Kin-Chun Luk; Steven Gregory Mischke; Hongmao Sun; Peter Michael Wovkulich
Archive | 2004
Jianping Cai; Robert Alan Goodnow
Archive | 2003
Jianping Cai; Nikolaos Dimoudis; Konrad Honold; Kin-Chun Luk; Stefan Scheiblich; Hilke Sudergat; Georg Tiefenthaler; Oliver Tonn
Archive | 2008
David Robert Bolin; Jianping Cai; Robert Alan Goodnow
Archive | 2007
John Frederick Boylan; Jianping Cai; Nader Fotouhi; Paul Gillespie; Jr. Robert Alan Goodnow; Kang Le; Christophe Michoud
Archive | 2004
Jianping Cai; Robert Alan Goodnow