Chinese Chemical Letters

Synthesis and biological evaluation of 5′-phenyl-3′ H-spiro-[indoline-3, 2′-[1, 3, 4] oxadiazol]-2-one analogs

HQ Liu, DC Wang, F Wu, W Tang, PK Ouyang

Index: Liu, Hua-Quan; Wang, De-Cai; Wu, Fei; Tang, Wei; Ouyang, Ping-Kai Chinese Chemical Letters, 2013 , vol. 24, # 10 p. 929 - 933

Full Text: HTML

Citation Number: 2

Abstract

Abstract 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 10 compounds investigated, 1k showed good binding affinities to Bcl-xL and Mcl-1, with inhibition constants of 8.9 μmol/L and 3.4 μmol/L, respectively. ...