Selective cytotoxicity of oxysterols through structural modulation on rings A and B. Synthesis, in vitro evaluation, and SAR

…, JN Moreira, S Simões, ML Sá e Melo

Index: Carvalho, Joao F. S.; Silva, M. Manuel Cruz; Moreira, Joao N.; Simoes, Sergio; Sa E Melo, M. Luisa Journal of Medicinal Chemistry, 2010 , vol. 53, # 21 p. 7632 - 7638

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Citation Number: 25

Abstract

Chemically diverse oxysterols were prepared and evaluated for cytotoxicity, aiming to push forward potency and selectivity. They were tested against seven cancer (HT-29, HepG2, A549, PC3, LAMA-84, MCF-7, and SH-SY5Y) and two noncancerous cell lines (ARPE-19 and BJ). The influence of the oxidation pattern on rings A and B was studied. Oxygen functionalities on ring B, such as oxo, oxime, acetamide, acetate, and alkoxy, were ...