58690-18-9Relevant academic research and scientific papers
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.
Synthesis of functionalized pyrroloindolines: Via a visible-light-induced radical cascade reaction: Rapid synthesis of (±)-flustraminol B
Wu, Kui,Du, Yuliu,Wei, Zheng,Wang, Ting
supporting information, p. 7443 - 7446 (2018/07/13)
The development of visible-light-induced synthesis of functionalized pyrroloindolines via a radical cascade reaction is reported. The reaction shows a broad substrate scope and highlights the mild nature of the reaction conditions. A range of substitutions on indole aromatic rings and N-centers is well tolerated, including a free allylic alcohol. Relying on the strategy, a rapid synthesis of (±)-flustraminol B was achieved.
Indole compound having antiviral activity
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Paragraph 0192; 0193; 0194; 0200; 0201; 0202, (2017/09/19)
The invention discloses an indole compound represented by general formula (I), and pharmaceutically acceptable salts thereof, and also discloses a preparation method of above compounds, and a medicinal composition of the compounds. The compounds have obvious anti-HIV activity and anti-influenza virus activity, and can be used for preparing anti-HIV or anti-influenza virus medicines or healthcare products.
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.).
Use of N-alkylindole compounds in preparation of anti-influenza virus medicines
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Paragraph 0193, (2017/09/19)
The invention discloses an application of indole compounds represented by general formula (I), and derivatives and pharmaceutically acceptable salts thereof in the preparation of anti-influenza virus medicines or healthcare products, and also discloses a preparation method of the compounds, and an application of medicinal compositions containing the compounds in the preparation of the anti-influenza virus medicines or healthcare products.
Bisindolyl maleimide derivative and preparation method and application thereof
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Paragraph 0197; 0198, (2017/01/02)
The invention provides a bisindolyl maleimide derivative and a preparation method and application thereof. The bisindolyl maleimide derivative has an excellent alpha-glucosidase inhibition effect and can be used for preventing and treating diabetes.
Bisindolylmaleimide derivative, and preparation method and use thereof
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Paragraph 0200; 0201, (2017/04/03)
The invention provides a bisindolylmaleimide derivative, and a preparation method and a use thereof. The bisindolylmaleimide derivative has a good tumor treatment effect, especially has a good treatment effect on some drug-resistant tumors, and can realize accurate treatment of the drug-resistant tumors.
Synthesis and pharmacological evaluation of (indol-3-yl)alkylamides as potent analgesic agents
Fouchard,Marchand,Le Baut,Emig,Nickel
, p. 814 - 824 (2007/10/03)
A series of (indol-3-yl)alkylamides was synthesized and evaluated for analgesic activity. Two N-(pyridin-4-yl)acetamides, compounds 24 and 25, bearing benzyl or 4-fluorobenzyl moieties in 1-position of indole ring exhibited promising analgesic properties (ED50 = 8.1 and 11 mg/kg p.o., respectively), being as potent as the reference drugs flupirtine (CAS 56995-20-1), ibuprofen (CAS 15687-27-1) and diclofenac (CAS 15307-86-5). The two test compounds were tested for their anti-inflammatory activity by carrageenin-induced edema in rat paw test. 4-Fluorobenzyl derivative 25 whose ID50 was 0.085 ± 0.021 mmol/kg was selected as a lead compound for further pharmacomodulation.
A ONE-STEP CONVERSION OF CERTAIN INDOLE AND PYRROLE GLYOXYLIC ACID ESTERS TO THE CORRESPONDING ACETATES
Demopoulos, Vassilis J.
, p. 2585 - 2594 (2007/10/02)
In this study, a catalytic hydrogen transfer type of hydrogenolysis was developed for the one step conversion of ethyl indole-3-, pyrrole-2- and pyrrole-3-glyoxalates to the corresponding acetates.The structural requirements for this hydrogenolysis were also investigated.
