Antitumor and chemopreventive effects of a clomiphene analog, MDL 103,323, in mammary carcinoma.
ANTICANCER RESEARCH(1996)
摘要
MDL 103,323, an enclomiphene analog, was tested for binding to the estrogen receptor, inhibition of human tumor xenografts and prevention of carcinogen-induced mammary tumors. MDL 103,323 had 5-6 fold greater affinity for the human estrogen receptor than did either tamoxifen or enclomiphene. Consistent with enhanced binding affinity, MDL 103,323 was more potent against MCF-7 cell proliferation and MCF-7 xenografts in nude mice were inhibited almost completely by MDL 103,323 doses greater than or equal to 0.02 mg/mouse/day (ED(50) (sic) 0.01 mg/mouse/day). N-methylnitrosourea induced rat mammary carcinomas were inhibited by greater than or equal to 50% at 0.003 mg/kg daily and by 90% at 0.1 mg/kg/day. The antitumor potency and efficacy of MDL 103,323 are striking and further evaluation of the compound for potential clinical utility is warranted.
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关键词
breast cancer,triphenylethylene,clomiphene,tamoxifen,chemoprevention,human xenografts,mammary carcinoma
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