On March 15, 2017, Liu, Tingting; Wan, Yichao; Liu, Renshuai; Ma, Lin; Li, Minyong; Fang, Hao published an article.COA of Formula: C6H5ClN2O4S The title of the article was Design, synthesis and preliminary biological evaluation of indole-3-carboxylic acid-based skeleton of Bcl-2/Mcl-1 dual inhibitors. And the article contained the following:
The B-cell lymphoma-2 (Bcl-2) family proteins are attractive targets for cancer therapy. In the previous work, the structure-activity relationship of WL-276 was studied. According to the results, rhodanine derivatives show potent binding affinity for Bcl-2 and Mcl-1 protein and show weaker activity against Bcl-XL protein. Based on the previous results, a new class of indole-3-carboxylic acid-based derivatives were designed and synthesized as Bcl-2/Mcl-1 dual inhibitors. Among them, compound I has a Ki value of 0.26 μM for Bcl-2 protein and is better than WL-276. Furthermore, it inhibits the myeloid cell leukemia sequence 1 (Mcl-1) protein with a Ki value of 72 nM. Especially, compound II can selectively acting on Bcl-2 and Mcl-1 protein but not Bcl-XL protein, which has great significance for developing dual inhibitors targeting Bcl-2 and Mcl-1 protein, as well as specific antitumor abilities in cells. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).COA of Formula: C6H5ClN2O4S
The Article related to indolecarboxylate bcl2 mcl1 inhibitor antitumor neoplasm, anti-tumor, bcl-2/mcl-1, indole-3-carboxylic acid-based derivatives, inhibitors, Pharmacology: Structure-Activity and other aspects.COA of Formula: C6H5ClN2O4S
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics