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Gusakov EA , Topchu IA , Mazitova AM , Dorogan IV , Bulatov ER , Serebriiskii IG , Abramova ZI , Tupaeva IO , Demidov OP , Toan DN , Lam TD , Bang DN , Boumber YA , Sayapin YA , Minkin VI
Design, synthesis and biological evaluation of 2-quinolyl-1,3-tropolone derivatives as new anti-cancer agents
Rsc Advances. 2021 Feb;11(8) :4555-4571
PMID: WOS:000612191100034   
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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.
Notes
Gusakov, Evgeniy A. Topchu, Iuliia A. Mazitova, Aleksandra M. Dorogan, Igor, V Bulatov, Emil R. Serebriiskii, Ilya G. Abramova, Zinaida, I Tupaeva, Inna O. Demidov, Oleg P. Duong Ngoc Toan Tran Dai Lam Duong Nghia Bang Boumber, Yanis A. Sayapin, Yurii A. Minkin, Vladimir, I 2046-2069