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JOURNALS // Mendeleev Communications // Archive

Mendeleev Commun., 2021 Volume 31, Issue 5, Pages 662–663 (Mi mendc1015)

This article is cited in 4 papers

Communications

Antitumor activity of phaeosphaeride A modified with nitrogen heterocyclic groups

S. A. Zakharenkovaa, V. V. Abzianidzea, N. I. Moiseevab, D. S. Lukinaa, L. S. Chistyia, D. V. Krivorotova, Yu. G. Trishinc

a Research Institute of Hygiene, Occupational Pathology and Human Ecology, Leningrad region, Russian Federation
b N.N. Blokhin National Medical Research Center of Oncology, Moscow, Russian Federation
c Saint-Petersburg State University of Industrial Technologies and Design, St. Petersburg, Russian Federation

Abstract: New C(6)-derivatives of natural phaeosphaeride A (PPA) modified with pharmacophoric nitrogen heterocyclic groups have been synthesized. The reaction of 1,2,4-triazole with PPA mesylate produced both the product of the expected substitution of the methanesulfonate group and the PPA derivative with two 1,2,4-triazole groups: at the C(6) atom and the exocyclic C=C bond. The synthesized compounds, with the exception of those containing two 1,2,4-triazole groups, are superior in cytotoxic activity to the original phaeosphaeride and the positive control, etoposide.

Keywords: antitumor activity, phaeosphaeride A, N-heterocyclic compounds, sulfides, natural products, in vitro studies, anticancer agents, etoposide.

Language: English

DOI: 10.1016/j.mencom.2021.09.023



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