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

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

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

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. This journal is

Original languageEnglish (US)
Pages (from-to)4555-4571
Number of pages17
JournalRSC Advances
Volume11
Issue number8
DOIs
StatePublished - Jan 22 2021

ASJC Scopus subject areas

  • Chemistry(all)
  • Chemical Engineering(all)

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