Jhingran, Akhil G. ; Gupta, R. C. ; Ray, Suprabhat ; Agarwal, A. K. ; Singh, M. M. ; Anand, Nitya (1983) Studies in antifertility agents — part XLI: secosteroids — X: syntheses of various stereoisomers of (±) 2,6β-diethyl-7α-ethynyl-3-(p-hydroxyphenyl)-trans-bicyclo[4.3.0]nonan-7β-ol Steroids, 42 (6). pp. 627-634. ISSN 0039-128X
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Official URL: http://www.sciencedirect.com/science/article/pii/0...
Related URL: http://dx.doi.org/10.1016/0039-128X(83)90126-5
Abstract
The syntheses of (+/-) 2 alpha,6 beta -diethyl-7 alpha -ethynyl-3 alpha-(p-hydroxyphenyl)-trans- bicyclo[4.3.0]nonan-7 beta-ol (8), (+/-)2 beta,6 beta-diethyl-7 alpha-ethynyl-3 beta-(p-methoxy-phenyl)-trans-bicyclo[4.3.0]nonan-7 beta-ol 12 and (+/-) 2 alpha,6 beta-diethyl-7 alpha-ethynyl-3 beta-(p-hydroxyphenyl)- trans-bicyclo[4.3.0]nonan-7 beta-ol (18) and their derivatives, which are essentially B-seco-steroids having cis-anti-trans, cis-syn-trans and trans-anti-trans geometries have been carried out. A study of their antiimplantation activities (AI) and receptor binding affinities (RBA) show that trans-anti-trans compounds are biologically most potent, followed by the corresponding cis-anti-trans and cis-syn-trans compounds. The most potent compound 18 is active at 1 mg/kg in rats. Introduction of 7 alpha-ethynyl group increases their AI activity; however, no significant effect on their RBA is observed.
| Item Type: | Article |
|---|---|
| Source: | Copyright of this article belongs to Elsevier Science. |
| ID Code: | 96859 |
| Deposited On: | 11 Feb 2013 06:36 |
| Last Modified: | 11 Feb 2013 06:36 |
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