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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 Adv. 2021 Feb;11(8) :4555-4571
PMID: 33996031 PMCID: PMC8121267 URL: https://www.ncbi.nlm.nih.gov/pubmed/33996031
AbstractTropolones 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.
NotesGusakov, 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 Toan, Duong Ngoc Lam, Tran Dai Bang, Duong Nghia Boumber, Yanis A Sayapin, Yurii A Minkin, Vladimir I eng P30 CA006927/CA/NCI NIH HHS/ P30 CA060553/CA/NCI NIH HHS/ R01 CA218802/CA/NCI NIH HHS/ R21 CA223394/CA/NCI NIH HHS/ England RSC Adv. 2021;11(8):4555-4571. doi: 10.1039/d0ra10610k. Epub 2021 Jan 22.