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Design, synthesis and biological evaluation of 2-quinolyl-1,3-tropolone derivatives as new anti-cancer agents

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Abstract

Tropolones are promising organic compounds that can have important biologic effects. We developed a series of new 2-quinolyl-1,3-tropolones derivatives that were prepared by the acid-catalyzed reaction of 4,7-dichloro-2-methylquinolines with 1,2-benzoquinones. 2-Quinolyl-1,3-tropolones have been synthesized and tested for their anti-proliferative activity against several human cancer cell lines. Two compounds (3d and mixture B of 3i–k) showed excellent activity against six cancer cell lines of different tissue of origin. The promising compounds 3d and mixture B of 3i–k also demonstrated induction of apoptotic cell death of ovarian cancer (OVCAR-3, OVCAR-8) and colon cancer (HCT 116) cell lines and affected ERK signaling. In summary, 2-quinolyl-1,3-tropolones are promising compounds for development of effective anticancer agents.

Graphical abstract: Design, synthesis and biological evaluation of 2-quinolyl-1,3-tropolone derivatives as new anti-cancer agents

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Supplementary files

Article information


Submitted
17 Dec 2020
Accepted
12 Jan 2021
First published
22 Jan 2021

This article is Open Access

RSC Adv., 2021,11, 4555-4571
Article type
Paper

Design, synthesis and biological evaluation of 2-quinolyl-1,3-tropolone derivatives as new anti-cancer agents

E. A. Gusakov, I. A. Topchu, A. M. Mazitova, I. V. Dorogan, E. R. Bulatov, I. G. Serebriiskii, Z. I. Abramova, I. O. Tupaeva, O. P. Demidov, D. N. Toan, T. D. Lam, D. N. Bang, Y. A. Boumber, Y. A. Sayapin and V. I. Minkin, RSC Adv., 2021, 11, 4555
DOI: 10.1039/D0RA10610K

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