20950-13-4Relevant articles and documents
Design, synthesis and biological evaluation of 3-aryl-rhodanine benzoic acids as anti-apoptotic protein Bcl-2 inhibitors
Fu, Huansheng,Hou, Xuben,Wang, Lei,Dun, Yanyan,Yang, Xinying,Fang, Hao
, p. 5265 - 5269 (2015)
A new class of 3-aryl-rhodanine benzoic acid derivatives were designed, synthesized, and evaluated for their inhibition activities against anti-apoptotic Bcl-2 proteins. The potent compounds 33 and 41 bound to Bcl-2 with submicromolar Ki values and had selectivities to Bcl-2/Mcl-1 over Bcl-xL. In addition, they exhibited obvious antiproliferative activities in three human tumor cell lines (MDA-MB-231, K562 and PC-3).
3. 5 - disubstituted the rhodanine class anti-withers apoptotic protein Bcl - 2 inhibitor and preparation method and application
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Paragraph 0158-0159, (2017/08/25)
The invention discloses a 3,5-disubstituted rhodanine anti-apoptosis protein Bc1-2 inhibitor as well as preparation method and an application thereof. The compound has a structure of a general formula I. The compound disclosed by the invention has high inhibitory activity on Bc1-2 and can be used for preparation of medicines for preventing or treating related mammal diseases caused by abnormal expression of anti-apoptosis protein Bc1-2. The invention also relates to a pharmaceutical application of a composition of the compound with the structure of the general formula I. The structural formula is as shown in the specification.