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

2-喹啉-1,3-托酚酮衍生物的设计、合成及新型抗癌药物的生物活性评价

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作者:Evgeniy A Gusakov #, Iuliia A Topchu #, Aleksandra M Mazitova #, Igor V Dorogan, Emil R Bulatov, Ilya G Serebriiskii, Zinaida I Abramova, Inna O Tupaeva, Oleg P Demidov, Duong Ngoc Toan, Tran Dai Lam, Duong Nghia Bang, Yanis A Boumber, Yurii A Sayapin, Vladimir I Minkin

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.

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