Biological Evaluation of Dipyrromethanes in Cancer Cell Lines: Antiproliferative and Pro-apoptotic Properties

0476572 - ÚEB 2018 RIV DE eng J - Journal Article
Jorda, Radek - Lopes, S. M.M. - Řezníčková, Eva - Kryštof, Vladimír - Pinho e Melo, T. M.V.D.
Biological Evaluation of Dipyrromethanes in Cancer Cell Lines: Antiproliferative and Pro-apoptotic Properties.
ChemMedChem. Roč. 12, č. 9 (2017), s. 701-711. ISSN 1860-7179. E-ISSN 1860-7187
R&D Projects: GA MŠMT(CZ) LO1204
Institutional support: RVO:61389030
Keywords : anticancer agents * apoptosis * cell cycle * cytotoxicity * dipyrromethanes
OECD category: Oncology
Impact factor: 3.009, year: 2017

Functionalized dipyrromethanes were synthesized by hetero-Diels–Alder reactions of nitroso- and azoalkenes and screened for their in vitro activity as anticancer agents. The studied dipyrromethanes were tested against leukemia and lymphoma cell lines, and showed GI 50 values in the mid-micromolar range. The pro-apoptotic 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 effects on the cell cycle are described. The latter compound was found to decrease the S-phase cell population in a dose-dependent manner and to irreversibly block cells in the G 2 /M phase.
Permanent Link: http://hdl.handle.net/11104/0273047