58690-18-9Relevant articles and documents
Chemical profiling of HIV-1 capsid-targeting antiviral PF74
Casey, Mary C.,Do, Ha T.,Du, Haijuan,Hachiya, Atsuko,Kirby, Karen A.,Sahani, Rajkumar Lalji,Sarafianos, Stefan G.,Tedbury, Philip R.,Vernekar, Sanjeev Kumar V.,Wang, Lei,Wang, Zhengqiang,Xie, Jiashu,Zhang, Huanchun
supporting information, (2020/05/19)
The capsid protein (CA) of HIV-1 plays essential roles in multiple steps of the viral replication cycle by assembling into functional capsid core, controlling the kinetics of uncoating and nuclear entry, and interacting with various host factors. Targetin
Novel synthetic bisindolylmaleimide alkaloids inhibit STAT3 activation by binding to the SH2 domain and suppress breast xenograft tumor growth
Li, Xia,Ma, Hongguang,Li, Lin,Chen, Yifan,Sun, Xiao,Dong, Zizheng,Liu, Jing-Yuan,Zhu, Weiming,Zhang, Jian-Ting
, p. 2469 - 2480 (2018/05/14)
Signal transducer and activator of transcription 3 (STAT3) is constitutively activated in malignant tumors and plays important roles in multiple aspects of cancer aggressiveness. Thus, targeting STAT3 promises to be an attractive strategy for the treatment of advanced metastatic tumors. Bisindolylmaleimide alkaloid (BMA) has been shown to have anti-cancer activities and was thought to suppress tumor cell growth by inhibiting protein kinase C. In this study, we show that a newly synthesized BMA analog, BMA097, is effective in suppressing tumor cell and xenograft growth and in inducing spontaneous apoptosis. We also provide evidence that BMA097 binds directly to the SH2 domain of STAT3 and inhibits STAT3 phosphorylation and activation, leading to reduced expression of STAT3 downstream target genes. Structure activity relationship analysis revealed that the hydroxymethyl group in the 2,5-dihydropyrrole-2,5-dione prohibits STAT3 inhibitory activity of BMA analogs. Altogether, we conclude that the synthetic BMA analogs may be developed as anti-cancer drugs by targeting and binding to the SH2 domain of STAT3 and inhibiting the STAT3 signaling pathway.
Application of N-alkylindole compound to preparation of anti-HIV (Human Immunodeficiency Virus) medicaments
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Paragraph 0193, (2017/09/29)
The invention discloses an indole compound shown as a general formula (I), and application of a pharmaceutically-acceptable salt of the indole compound to preparation of anti-HIV medicaments or health care products, and discloses a preparation method of the compound and application of a medicinal composition containing the compound to preparation of anti-HIV medicaments or health care products. (The structural formula of the compound is shown in the description.).