Design and synthesis of 21-alkynylaryl pregnenolone derivatives and evaluation of their anticancer activity

Bioorg Med Chem. 2014 Dec 15;22(24):6980-8. doi: 10.1016/j.bmc.2014.10.012.

György Szalóki ¹, Athanasia Pantzou ¹, Kyriakos C Prousis ¹, Olga Mavrofrydi ², Panagiota Papazafiri ², Theodora Calogeropoulou ³

Affiliations

1 Institute of Biology, Medicinal Chemistry and Biotechnology, National Hellenic Research Foundation, 48 Vas. Constantinou Avenue, Athens 11635, Greece.
2 University of Athens, Department of Biology, Division of Animal and Human Physiology, Panepistimiopolis, Athens 15784, Greece.
3 Institute of Biology, Medicinal Chemistry and Biotechnology, National Hellenic Research Foundation, 48 Vas. Constantinou Avenue, Athens 11635, Greece. Electronic address: tcalog@eie.gr.

PMID: 25456391 DOI: 10.1016/j.bmc.2014.10.012

Abstract

A series of novel C21-alkynylaryl derivatives of pregnenolone were synthesized and screened for Anticancer activity against a panel of seven human Cancer cell lines (LNCaP, A549, MCF7, HeLa, A431, HepG2, HT29). The data revealed that these compounds can be potential antitumour agents against the specific cell models. Compound 6f bearing a 2-trifluoromethylphenyl group displayed improved cytotoxicity towards all Cancer cell lines used. A431 cells were the most sensitive with derivatives 6e-6h bearing electron withdrawing substituents exhibiting high potency with IC50 values ranging between 2.18 and 0.54μM and drastic inhibition of the prosurvival PI3K-Akt/PKB pathway.

Keywords

Alkynylaryl derivatives; Anticancer activity; Pregnenolone.

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