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https://open.uns.ac.rs/handle/123456789/15714
Title: | X-ray crystal structure of 10β-hydroxy-4β,5β-epoxyestr-1-en3,17-dione and antitumor activity of its congeners | Authors: | Milić, Dragan Kapor A. Markov B. Ribar B. Strümpel M. Juranić Z. Gašić M. Šolaja B. |
Issue Date: | 1-Jan-1999 | Journal: | Molecules | Abstract: | Based on the biological properties of epoxyquinols from natural sources, the title compound was synthesised as a potential antitumor agent. Its molecular structure was partially confirmed by NMR studies. The detailed structure was established by X-ray analysis revealing two symmetry independent molecules in the asymmetric unit each consisting of four fused rings with the C(10) β-oriented hydroxy group and β-oriented O atom bridging C(4) and C(5). The conformation of A ring in both conformers A and B is boat (B3,6 ), while rings B and C are chairs (1C4) and the five-membered D ring is in an envelope (E2) conformation. The in vitro antitumor activity of title compound and its 17β-acetoxy analogue against HeLa and Fem-x cells revealed IC50 values of 5.7 and 7.1 μM, and 2.25 and 1.58 μM, respectively. Corresponding quinols were tested on 47 cell lines with 10β-hydroxy-17β-acetoxyestra-1,4-dien-3-one being most active against leukemia SR cells (GI50 = 0.17 μM). | URI: | https://open.uns.ac.rs/handle/123456789/15714 | ISSN: | 14203049 | DOI: | 10.3390/41200338 |
Appears in Collections: | POLJF Publikacije/Publications |
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