Add time:07/19/2019         Source:sciencedirect.com

Twelve 17-(2′-oxazolyl)- and 17-(2′-thiazolyl)-androsta-5,16-diene derivatives were designed and synthesized from 3β-acetoxy-pregna-5,16-dien-20-one (1b) as inhibitors of 17α-hydroxylase-C17,20-lyase (P45017α). Potent inhibitors of this enzyme could be of value as treatment of prostate cancer. Two substituents (methyl and phenyl) were introduced either at their 4′- or 5′-position in order to investigate their structure–activity relationship. Due to the 16,17-double bond, 17-thiazoles were generally obtained in low yield. The pharmacological results showed that the compounds containing 17-(2′-oxazolyl) (14c) and 17-(2′-thiazolyl) (8c) (41.5%) demonstrated reasonable inhibition against P45017α. Their 3-acetate (13c and 7c) were less potent than their 3-OH counterparts. The introduction of a phenyl or methyl group generally decreased inhibitory activity. Surprisingly, 17-(5′-methyl-2′-thiazolyl) (12a) was the most potent compound in this series and was almost as potent as L-39, which has good antitumor activity.

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