Abstract

STRUCTURE–ACTIVITY RELATIONSHIPS FOR A SERIES OF PHENYL (MORPHOLINO) METHANETHIONE DERIVATIVES: CYTOTOXICITY AGAINST ARTEMIA SALINA AND CANCER CELL LINES

Agnimonhan F. Hyacinthe*, Glinma Bienvenu, Ahoussi A. Léon, Kpoviessi D. S. Salomé, Accrombessi C. Georges and Gbaguidi A. Fernand

ABSTRACT

A series of phenyl (morpholino) methanethione derivatives (a-h) has been evaluated for antiproliferative activity vitro against MCF-7 and HCT-116 cancer cells by the MTT assay and toxicity on the larvae of Artemia salina Leach. From the toxicity studies and structural activity relationship of compounds (a-h), it is clear that mesomeric donor effect groups on benzene ring have increased actively this toxicity. Moreover, for cytotoxicity studies on MCF-7 and HCT-116 cancer cells in breast and colon cancer respectively, the compounds (a) and (f) have showed an interesting activity with 100 μM of (f) on MCF-7 cells (35.7 ± 3.1%) and 100 μM of the compound (a) on the HCT-116 cells (58.1 ± 1.5%). A cytotoxicity on MCF-7 of these compounds has expressed a toxicity on the larvae of Artemia salina. This does phenyl (morpholino) methanethione derivatives a potential source of anti-cancer molecules.

Keywords: Artemia salina Leach, MCF-7, HTC-116, phenyl (morpholino) methanethione derivatives.