252919-04-3Relevant academic research and scientific papers
Studies of CDK 8/19 inhibitors: Discovery of novel and selective CDK8/19 dual inhibitors and elimination of their CYP3A4 time-dependent inhibition potential
Fujimoto, Jun,Hirayama, Takaharu,Hirata, Yasuhiro,Hikichi, Yukiko,Murai, Saomi,Hasegawa, Maki,Hasegawa, Yuka,Yonemori, Kazuko,Hata, Akito,Aoyama, Kazunobu,Cary, Douglas R.
, p. 3018 - 3033 (2017)
In this article, synthetic studies around a pyridylacrylamide-based hit compound (1), utilizing structure-based drug design guided by CDK8 docking models, is discussed. Modification of the pendant 4-fluorophenyl group to various heteroaromatic rings was c
TARGETED POLYMERIC PRODRUGS CONTAINING MULTIFUNCTIONAL LINKERS
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Page/Page column 73, (2008/06/13)
The present invention provides single chain antibody-directed polymeric prodrugs containing multifunctional linkers. Methods of making the polymeric delivery systems and methods of treating mammals using the same are also disclosed.
Rational design, synthesis and structure-Activity relationships of a cyclic succinate series of TNF-α converting enzyme inhibitors. Part 1: Lead identification
Xue, Chu-Biao,He, Xiaohua,Roderick, John,Corbett, Ronald L.,Duan, James J.-W.,Liu, Rui-Qin,Covington, Maryanne B.,Newton, Robert C.,Trzaskos, James M.,Magolda, Ronald L.,Wexler, Ruth R.,Decicco, Carl P.
, p. 4293 - 4297 (2007/10/03)
Rational design based on the broad spectrum MMP inhibitor CGS 27023A led to the identification of a novel series of cyclic succinate TACE inhibitors. As a mixture of two enantiomers, the lead compound 17b exhibited potent enzyme activity (IC50=
