期刊
MOLECULES
卷 26, 期 7, 页码 -出版社
MDPI
DOI: 10.3390/molecules26072066
关键词
3+2 cycloaddition; pyrrolo fused (iso)quinoline; anticancer; tubulin polymerization inhibitor; molecular docking
资金
- Romanian Ministry of Education and Research, CNCS-UEFISCDI within PNCDI III [PN-III-P4-ID-PCE-2020-0371]
- European Social Fund through the Operational Programme Human Capital 2014-2020 [POCU/380/6/13/123623]
A series of new cyano-substituted derivatives with pyrrolo[1,2-a]quinoline and pyrrolo[2,1-a]isoquinoline scaffolds were synthesized through [3 + 2] cycloaddition reactions. Compound 9a showed potent anticancer activity across a range of human cancer cell lines, with in vitro assays and molecular docking revealing its tubulin interaction properties.
Several new cyano-substituted derivatives with pyrrolo[1,2-a]quinoline and pyrrolo[2,1-a]isoquinoline scaffolds were synthesized by the [3 + 2] cycloaddition of (iso)quinolinium ylides to fumaronitrile. The cycloimmonium ylides reacted in situ as 1,3-dipoles with fumaronitrile to selectively form distinct final compounds, depending on the structure of the (iso)quinolinium salt. Eleven compounds were evaluated for their anticancer activity against a panel of 60 human cancer cell lines. The most potent compound 9a showed a broad spectrum of antiproliferative activity against cancer cell lines representing leukemia, melanoma and cancer of lung, colon, central nervous system, ovary, kidney, breast and prostate cancer. In vitro assays and molecular docking revealed tubulin interaction properties of compound 9a.
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