【摘 要】
：
A series of 5’-phenyl-3’H-spiro[indoline-3,2’-[1,3,4]thiadiazol]-2-one analogs were synthesized and their Bcl-2 protein inhibitory activities were studied. T
【机 构】
：
School of Pharmaceutical Science,Nanjing University of Technology,College of Life Science and Pharma
【出 处】
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Chinese Chemical Letters
论文部分内容阅读
A series of 5’-phenyl-3’H-spiro[indoline-3,2’-[1,3,4]thiadiazol]-2-one analogs were synthesized and their Bcl-2 protein inhibitory activities were studied. The lead compound was originally identifed using a fluorescence polarization-based competitive binding assay. Among the 1’ compounds investigated, 1k showed good binding affnities to Bcl-xL and Mcl-1, with inhibition constants of 8.9 μmol/L and3.4 μmol/L, respectively. While compound 1c achieved tight binding affnities to Bcl-xL(Ki = 0.16 μmol/L), has the potential to be a new lead compound.
A series of 5’-phenyl-3’H-spiro [indoline-3,2 ’- [1,3,4] thiadiazol] -2-one analogs were synthesized and their Bcl-2 protein inhibitory activities were studied. The lead compound was originally identified using a fluorescence polarization-based competitive binding assay. Among the 1 ’compounds investigated, 1k showed good binding affnities to Bcl-xL and Mcl-1 with inhibition constants of 8.9 μmol / L and 3.4 μmol / L, While compound 1 achieved very tight binding affnities to Bcl-xL (Ki = 0.16 μmol / L), has the potential to be a new lead compound.
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