Chen, Jianfang; Zhou, Haibin; Aguilar, Angelo; Liu, Liu; Bai, Longchuan; McEachern, Donna; Yang, Chao-Yie; Meagher, Jennifer L.; Stuckey, Jeanne A.; Wang, Shaomeng published the artcile< Structure-Based Discovery of BM-957 as a Potent Small-Molecule Inhibitor of Bcl-2 and Bcl-xL Capable of Achieving Complete Tumor Regression>, COA of Formula: C7H7ClO4S2, the main research area is pyrrole carboxylic acid preparation Bcl2 BclxL inhibitor SAR.
Bcl-2 and Bcl-xL antiapoptotic proteins are attractive cancer therapeutic targets. We have previously reported the design of 4,5-diphenyl-1H-pyrrole-3-carboxylic acids as a class of potent Bcl-2/Bcl-xL inhibitors. In the present study, we report our structure-based optimization for this class of compounds based upon the crystal structure of Bcl-xL complexed with a potent lead compound Our efforts accumulated into the design of compound 30 (BM-957, I), which binds to Bcl-2 and Bcl-xL with Ki < 1 nM and has low nanomolar IC50 values in cell growth inhibition in cancer cell lines. Significantly, compound 30 achieves rapid, complete, and durable tumor regression in the H146 small-cell lung cancer xenograft model at a well-tolerated dose schedule. Journal of Medicinal Chemistry published new progress about Antitumor agents. 5335-40-0 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H7ClO4S2, COA of Formula: C7H7ClO4S2.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics