On January 1, 2017, Wan, Yichao; Liu, Tingting; Li, Xiaoxian; Chen, Chen; Fang, Hao published an article.Category: amides-buliding-blocks The title of the article was Improved binding affinities of pyrrolidine derivatives as Mcl-1 inhibitors by modifying amino acid side chains. And the article contained the following:
As an important member of anti-apoptotic Bcl-2 protein, myeloid cell leukemia sequence 1 (Mcl-1) protein is an attractive target for cancer therapy. In this study, a new series of pyrrolidine derivatives as Mcl-1 inhibitors were developed by mainly modifying the amino acid side chain of compound 1. Among them, compound 18 (Ki = 0.077 μM) exhibited better potent inhibitory activities towards Mcl-1 protein compared to pos. control Gossypol (Ki = 0.18 μM). In addition, compound 40 possessed good antiproliferative activities against PC-3 cells (Ki = 8.45 μM), which was the same as pos. control Gossypol (Ki = 7.54 μM). The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Category: amides-buliding-blocks
The Article related to pyrrolidine derivative preparation sar mcl1 inhibitor bcl2 apoptosis cancer, bcl-2, cancer, mcl-1, pyrrolidine, target, Pharmacology: Structure-Activity and other aspects.Category: amides-buliding-blocks
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