Document Report Card

ID: ALA1134552

Journal: J Med Chem

Title: Synthesis of cytotoxic 6E-hydroximino-4-ene steroids: structure/activity studies.

Authors: Deive N, Rodríguez J, Jiménez C.

Abstract: In an effort to determine the pharmaceutical utility and the structural requirements for activity against various tumor cell lines, several 6E-hydroximino-4-ene steroids with different side chains and degrees of unsaturation on ring A were synthesized in our laboratory. Evaluation of the synthesized compounds for cytotoxicity against P-388, A-549, HT-29, and MEL-28 tumor cells revealed that some important structural features are required for activity. The presence of a cholesterol-type side chain, which appears to play a major role in determining the biological activity, the existence of a ketone functionality at C-3, and an elevated degree of oxidation on ring A all result in higher bioactivity than other structural motifs.

CiteXplore: 11472215

DOI: 10.1021/jm010867n