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Bioorg Khim ; 38(4): 499-508, 2012.
Artículo en Ruso | MEDLINE | ID: mdl-23189566

RESUMEN

A number of 24-norbrassinolide biosynthetic precursors containing low polar functional groups (3beta3-OH, 3-keto-, delta2- or 2alpha,3alpha-epoxy-) in A-cycle and (22R,23R)-diol in the side chain has been prepared. Studies of these compounds as proliferation regulators in MCF-7 human breast cancer and LnCaP human prostate adenocarcinoma cells showed that most nonpolar (22R,23R)-derivatives effectively suppressed proliferation. Dependence of proliferation on concentration of studied compounds was found in human prostate carcinoma LnCaP cells (IC50 = 13-28 microM at 72 h of incubation in a medium containing 10% FBS; suppression of DNA biosynthesis). A number of compounds induced apoptosis (23-33%); arrested cell cycle in S- and G2/M-phases; and caused partial cells detachment during prolonged incubations.


Asunto(s)
Brasinoesteroides , Proliferación Celular/efectos de los fármacos , Esteroides Heterocíclicos , Apoptosis/efectos de los fármacos , Brasinoesteroides/síntesis química , Brasinoesteroides/química , Brasinoesteroides/farmacología , Femenino , Humanos , Células MCF-7 , Masculino , Esteroides Heterocíclicos/síntesis química , Esteroides Heterocíclicos/química , Esteroides Heterocíclicos/farmacología
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