1133784-43-6Relevant articles and documents
Synthesis and biological evaluation of 3,5-disubstituted-4-alkynylisoxozales as a novel class of HSP90 inhibitors
Sun, Jian,Lin, Cai,Qin, Xiaochu,Dong, Xiaoping,Tu, Zhengchao,Tang, Fei,Chen, Chaonan,Zhang, Jiancun
, p. 3129 - 3134 (2015)
Abstract A series of 3,5-disubstitute-4-alkynylisoxazole derivatives were designed and synthesized through palladium(II)-copper(I) catalyzed Sonogashira cross-coupling reaction of an alkynyl moiety and an isoxazole scaffold as novel HSP90 inhibitors. The resultant compounds displayed moderate to potent binding affinity to HSP90 proteins, and also demonstrated good cell growth inhibitory activity against various cancer cell lines (A549, K562, MCF-7, DU145 and Hela). Some compounds (18d, 18e, 19a, 19d, 20c and 20q) show similar or better binding affinity towards HSP90α and HSP90β comparing to NVP-AUY922. In addition, compounds 18e, 19a and 20q exhibited potent inhibitory activity against various human cancer cell lines.
A NOVEL 5-MEMBERED HETEROCYCLE DERIVATIVES AND MANUFACTURING PROCESS THEREOF
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Page/Page column 24-25, (2011/09/19)
Disclosed herein are a novel 5-membered heterocycle derivatives represented by Formula I, a tautomer, pharmaceutically approved salts thereof, prodrug of this compound, or pharmaceutically use. Accordingly this prevent invention, a novel 5-membered heterocycle derivatives, a tautomer, pharmaceutically approved salt, or prodrug show antitumoral activity. Thus, this compounds are useful in the treatment of tumor.
