Biological evaluation of dipyrromethanes in cancer cell lines: antiproliferative and proapoptotic properties.

Biological evaluation of dipyrromethanes in cancer cell lines: antiproliferative and proapoptotic properties.

ChemMedChem. 2017 Apr 05;:

Authors: Jorda R, Lopes S, Řezníčková E, Kryštof V, Pinho E Melo T

Abstract
Functionalized dipyrromethanes were synthesized by using hetero-Diels-Alder reactions of nitroso- and azo-alkenes and screened for their in vitro activity as anticancer agents. The studied dipyrromethanes were tested against leukemia and lymphoma cell lines and reached GI50 values in mid-micromolar ranges. Proapoptotic activities of two candidates, ((E)-1-(2'-ethoxycarbonylhydrazono-1'-benzyl-1H-tetrazol-5-yl)-5,5'-diethyldipyrromethane and (E)-1-(2'-p-nitrophenyl-2'-hydroxyiminoethyl)-5-phenyldipyrromethane, and their effect on the cell cycle is described. The latter showed decrease of S-phase cells population in a dose-dependent manner and irreversibly blocked cells in G2/M phase.

PMID: 28378923 [PubMed - as supplied by publisher]

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