Shi, Zhi-Bing; Zhao, Dan; Huang, Yan-Yan; Du, Yun; Cao, Xiang-Rong; Gong, Zhu-Nan; Zhao, Rui; Li, Jian-Xin published the artcile< Discovery, synthesis, and evaluation of small-molecule signal transducer and activator of transcription 3 inhibitors>, Electric Literature of 1524-40-9, the main research area is transcription factor STAT3 inhibitor anticancer antitumor benzoxazole benzenesulfonamide.
The signal transducer and activator of transcription 3 (STAT3) oncogene is a promising mol. target and its inhibitors have great potential as anticancer drugs. To identify novel and STAT3-selective inhibitors, a virtual screening based on Specs and Maybridge databases was conducted and a 6,6′-bibenzoxazole type small mol. with an inhibition constant Ki value of 494.32 nm to STAT3 was explored. Further, a novel series of compounds was synthesized and evaluated by a cell-based assay using human breast cancer cell lines, MDA-MB-468 and MCF-7 with or without constitutive expression of STAT3, resp. Several compounds displayed inhibitory activity and good selectivity. Several compounds also significantly inhibited STAT3 protein level and also displayed binding affinity for STAT3 that detected with flow injection anal.-quartz crystal microbalance (FIA-QCM) anal. system. The results provided a new lead for future design and development of potent STAT3 inhibitors. The synthesis of the target compounds was achieved using 4,4′-diamino-[1,1′-biphenyl]-3,3′-diol (3,3′-dihydroxybenzidine) as a starting material. The title compounds thus formed included N,N’-[6,6′-bibenzoxazole]-2,2′-diylbis[benzenesulfonamide] (I) and related substances, such asN-(2-benzoxazolyl)-2-methylbenzenesulfonamide.
Chemical & Pharmaceutical Bulletin published new progress about Animal oncogene Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 1524-40-9 belongs to class amides-buliding-blocks, and the molecular formula is C6H6FNO2S, Electric Literature of 1524-40-9.
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