A series of 5＇-phenyl-3＇H-spiro[indoline-3,2＇-[l,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 fluore...A series of 5＇-phenyl-3＇H-spiro[indoline-3,2＇-[l,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 10 compounds investigated, I k showed good binding affinities to Bcl-xL and Mcl-l, with inhibition constants of 8.9 μmol/L and 3.4 μmol/L, respectively. While compound lc achieved tight binding affinities to Bcl-xL （Ki= 0.16 μmol/L）, has the potential to be a new lead compound.展开更多
文摘A series of 5＇-phenyl-3＇H-spiro[indoline-3,2＇-[l,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 10 compounds investigated, I k showed good binding affinities to Bcl-xL and Mcl-l, with inhibition constants of 8.9 μmol/L and 3.4 μmol/L, respectively. While compound lc achieved tight binding affinities to Bcl-xL （Ki= 0.16 μmol/L）, has the potential to be a new lead compound.
