Gao, Dingding; Jin, Nan; Fu, Yixian; Zhu, Yueyue; Wang, Yujie; Wang, Ting; Chen, Yuehong; Zhang, Mingming; Xiao, Qiang; Huang, Min; Li, Yingxia published the artcile< Rational drug design of benzothiazole-based derivatives as potent signal transducer and activator of transcription 3 (STAT3) signaling pathway inhibitors>, Application In Synthesis of 623-50-7 , the main research area is breast cancer benzothiazole based derivative anticancer STAT3 drug design; Antitumor activity; Benzothiazole; Molecular docking; Rational design; STAT3 signaling pathway.
The cumulative evidence supports STAT3, a transcriptional mediator of oncogenic signaling, as a therapeutic target in cancer. The development of STAT3 inhibitors remain an active area of research as no inhibitors have yet to be approved for cancer treatment. In a continuing effort to develop more potent STAT3 inhibitors based on our previously identified hit compound 16w, a series of benzothiazole derivatives with unique binding mode in SH2 domain of STAT3 were designed, synthesized and biol. evaluated. Of note, compound B19 demonstrated excellent activity against IL-6/STAT3 signaling pathway with the IC50 value as low as 0.067娓璏 as determined by a luciferase reporter assay. Moreover, multiple compounds displayed potent antiproliferative activity against MDA-MB-468 and JAK2 mutant HEL cell lines. Further biochem. study using Western blot assay indicated that B19 blocked the phosphorylation of STAT3 at Tyr 705 and Ser 727 and thus suppressed STAT3-mediated gene expression of c-MYC and MCL-1. Simultaneously, it induced cancer cell G2/M phase arrest and apoptosis both in MDA-MB-468 and HEL cell lines. Finally, mol. docking study along with surface plasmon resonance (SPR) and fluorescence polarization (FP) assays disclosed the binding mode of B19 in STAT3 SH2 domain. Taken together, our finding suggests that B19 is a promising therapeutic STAT3 inhibitor for cancer treatment.
European Journal of Medicinal Chemistry published new progress about Acute erythroid leukemia. 623-50-7 belongs to class esters-buliding-blocks, and the molecular formula is C4H8O3, Application In Synthesis of 623-50-7 .
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