STRUCTURE-ACTIVITY-RELATIONSHIPS OF ESTROGENS - EFFECTS OF 14-DEHYDROGENATION AND AXIAL METHYL-GROUPS AT C-7, C-9 AND C-11
STRUCTURE-ACTIVITY-RELATIONSHIPS OF ESTROGENS - EFFECTS OF 14-DEHYDROGENATION AND AXIAL METHYL-GROUPS AT C-7, C-9 AND C-11
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DOI：
10.1016/0039-128x(83)90054-5
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发表时间：
1983-01-01
期刊：
影响因子：
2.7
通讯作者：
SEGALOFF, A
中科院分区：
文献类型：
--
作者：
GABBARD, RB;SEGALOFF, A
Compounds (30) were evaluated in the rat for uterotropic effects, inhibition of gonadotropin release and competitive displacement of (3H) estradiol-17.beta. from uterine cytosolic preparations. 7.alpha.-Methylestradiol-17.beta. was 150% as active as estradiol-17.beta. as an uterotropic agent. Estradiol-17.beta. was the most active inhibitor of gonadotropin release. 11.beta.-Methylestradiol-17.beta. had 124% of the activity of estradiol-17.beta. in displacing (3H) estradiol-17.beta. from the estrogen receptor. The 9.alpha.-methyl group considerably decreased the potency of estrogens in any of the 3 assays. The 14-dehydro modification was advantageous only in the estradiol-17.beta. 3-methyl ether series. Uterotropic activities and inhibition of gonadotropin release did not parallel. The best compound for inhibiting gonadotropin release, as compared to uterotropic activity, was estrone. The estrogen receptor assay data correlated fairly well with uterotropic assay data, but only for compounds having free 3-hydroxyl groups; even so, some exceptions were noted.
