Synthesis and biological activity of some D-ring modified estrone derivatives

Authors
Gupta, R Jindal, DP Borras, M Legros, N Leclercq, G
Citation
R. Gupta et al., Synthesis and biological activity of some D-ring modified estrone derivatives, I J CHEM B, 38(5), 1999, pp. 563-571
Citations number
15
Categorie Soggetti
Organic Chemistry/Polymer Science
Journal title
INDIAN JOURNAL OF CHEMISTRY SECTION B-ORGANIC CHEMISTRY INCLUDING MEDICINAL CHEMISTRY
ISSN journal
03764699 → ACNP
Volume
38
Issue
5
Year of publication
1999
Pages
563 - 571
Database
ISI
SICI code
0376-4699(199905)38:5<563:SABAOS>2.0.ZU;2-D
Abstract
3-Methoxy-17-aza-D-homo-1,3,5(10)-estratriene-16,17a-dione 3, 16, 17a-dioxo -17-aza-D-homo-1,3,5(10)-estratrien-3-yl acetate 12 and a series of related compounds have been synthesised from 3-methoxy-16-oximino-1,3,5 (10)-estra trien-17-one 1 and 3-hydroxy-16-oximino-1,3,5 (10)-estratrien-17-one 2, res pectively. The compounds 3 (DPJ-280), 14 (DPJ-369), 17 (DPJ-370), 18 (DPJ-3 54), 19 (DPJ-320), 21 (DPJ-321), 22 (DPJ-374) and (DPJ-284) have been evalu ated for their estrogenic/antiestrogenic effects and the compounds 3-7,8,9, 10,12,15,16,18,20,21,23 and 24 have been screened for antineoplastic activi ty at NCI, Bethesda.