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- Title
Synthesis and Biological Screening of New Cyano-Substituted Pyrrole Fused (Iso)Quinoline Derivatives.
- Authors
Al-Matarneh, Maria Cristina; Amărandi, Roxana-Maria; Mangalagiu, Ionel I.; Danac, Ramona; Piccialli, Vincenzo
- Abstract
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.
- Subjects
PYRROLE derivatives; QUINOLINE derivatives; BIOSYNTHESIS; PYRROLES; MOLECULAR docking; CENTRAL nervous system
- Publication
Molecules, 2021, Vol 26, Issue 7, p2066
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules26072066