Synthesis and Antiproliferative Activity Evaluation of Aryl(Hetaryl)Cyclopentenone Analogs of Combretastatin A-4


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Abstract

A series of previously unreported di- and triaryl(hetaryl)cyclopentenone derivatives were prepared using a convenient synthetic method and screened preliminarily for antitumor activity in four human cell lines, i.e., T-cell leukemia (Jurkat), lung adenocarcinoma (A-549), colon cancer (HCT-116), and breast adenocarcinoma (MCF-7). The most cytotoxic of the tested compounds was 2-(3,4,5-trimethoxyphenyl)-3-(4-methoxyphenyl) cyclopent-2-en-1-one. However, it was inactive against lymphocytic leukemia P388 in mice despite its cytotoxicity in in vitro tests.

About the authors

V. Z. Shirinyan

N. D. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences

Author for correspondence.
Email: shir@ioc.ac.ru
Russian Federation, 47 Leninskii Prosp, Moscow, 119991

A. I. Markosyan

Scientific and Technological Center of Organic and Pharmaceutical Chemistry, National Academy of Sciences of Armenia

Email: shir@ioc.ac.ru
Armenia, 26 Azatutyan Pr., 0014, Yerevan, 375014

M. A. Baryshnikova

N. N. Blokhin Russian Cancer Research Center, Russian Academy of Medical Sciences

Email: shir@ioc.ac.ru
Russian Federation, 23 Kashirskoe Shosse, Moscow, 115478

L. V. Yaminova

D. I. Mendeleev University of Chemical Technology of Russia

Email: shir@ioc.ac.ru
Russian Federation, 9 Miusskaya Pl., Moscow, 125047

A. G. L’vov

N. D. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences

Email: shir@ioc.ac.ru
Russian Federation, 47 Leninskii Prosp, Moscow, 119991

S. A. Gabrielyan

Scientific and Technological Center of Organic and Pharmaceutical Chemistry, National Academy of Sciences of Armenia

Email: shir@ioc.ac.ru
Armenia, 26 Azatutyan Pr., 0014, Yerevan, 375014


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