119720-84-2Relevant articles and documents
Thiazolidine derivatives or salts thereof as an active ingredient an inhibitor Pim
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Paragraph 0685; 0686, (2018/10/19)
PROBLEM TO BE SOLVED: To provide compounds which have excellent Pim inhibitory action and are useful as pharmaceuticals.SOLUTION: A compound is a thiazolidine derivative represented by the general formula (1) in the figure, or a salt thereof. (In the formula, X represents O or S; Rrepresents a hydrogen atom or a Calkyl group; Z, Z, Z, Z, Zand Zeach independently represent CH or N; Y represents an optionally substituted, divalent Caromatic hydrocarbon group or the like; Am represents a disubstituted amino group, or an optionally substituted, nitrogen-containing saturated heterocyclic group; and Rand Reach independently represent a hydrogen atom, a halogen atom, an alkyl group or the like.)
Synthesis and evaluation of a novel class Hsp90 inhibitors containing 1-phenylpiperazine scaffold
Jia, Jian-Min,Liu, Fang,Xu, Xiao-Li,Guo, Xiao-Ke,Jiang, Fen,Cherfaoui, Bahidja,Sun, Hao-Peng,You, Qi-Dong
supporting information, p. 1557 - 1561 (2014/03/21)
Previously, we identified 1-(2-(4-bromophenoxy)ethoxy)-3-(4-(2- methoxyphenyl)piperazin-1-yl)propan-2-ol (1) as a novel Hsp90 inhibitor with moderate activity through virtual screening. In this study, we report the optimization process of 1. A series of analogues containing the 1-phenylpiperazine core scaffold were synthesized and evaluated. The structure-activity relationships (SAR) for these compounds was also discussed for further molecular design. This effort afforded the most active inhibitor 13f with improved activity in not only target-based level, but also cell-based level compared with the original hit 1.
