1333256-98-6Relevant articles and documents
Synthesis and Evaluation of Aryl Quinolines as HIV-1 Integrase Multimerization Inhibitors
Jentsch, Nicholas G.,Hart, Alison P.,Hume, Jared D.,Sun, Jian,McNeely, Kaitlin A.,Lama, Chiyang,Pigza, Julie A.,Donahue, Matthew G.,Kessl, Jacques J.
, p. 1007 - 1012 (2018)
HIV-1 integrase multimerization inhibitors have recently been established as an effective class of antiretroviral agents due to their potent ability to inhibit viral replication. Specifically, quinoline-based inhibitors have been shown to effectively impair HIV-1 replication, highlighting the importance of these heterocyclic scaffolds. Pursuant of our endeavors to further develop a library of quinoline-based candidates, we have implemented a structure-activity relationship study of trisubstituted 4-arylquinoline scaffolds that examined the integrase multimerization properties of substitution patterns at the 4-position of the quinoline. Compounds consisting of substituted phenyl rings, heteroaromatics, or polycyclic moieties were examined utilizing an integrase aberrant multimerization in vitro assay. para-Chloro-4-phenylquinoline 11b and 2,3-benzo[b][1,4]dioxine 15f showed noteworthy EC50 values of 0.10 and 0.08 μM, respectively.
6H-benzopyrano[3,4-b]quinoline compounds as well as preparation method and application thereof
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Paragraph 0018; 0020; 0021; 0026, (2021/01/29)
The invention relates to new 6H-benzopyrano[3,4-b]quinoline compounds as well as a preparation method and application thereof in preparation of antitumor drugs. The chemical general formulas of the compounds are shown as structural formulas (I) and (II). In-vitro anti-tumor activity screening results show that the compounds represented by the formula I and the formula II have broad-spectrum anti-tumor activity, and have strong inhibition activity on human colorectal cancer (HCT116), human liver cancer (HepG2), human pancreatic cancer (SW1990), human ovarian cancer (A2780), human breast cancer(MCF7) and human cervical cancer (Hela). Compounds 7h and 7n have relatively strong anti-inhibition activity on a HepG2 cell line, and IC50 of the compounds is 0.58 [mu]M and 1.94 [mu]M respectively and is remarkably superior to that of a control drug irinotecan; a compound 7a has high selectivity on a Hela cell line, and IC50 is 4.37 [mu]M; and compounds 9h and 9i have strong inhibition effects on six tumor cell lines, and the IC50 values are 6.38-21.04 [mu]M and 5.12-23.31 [mu]M respectively. Therefore, the compounds can be used for preparing anti-tumor drugs.