Synthesis and antitumor activity of new d-seco and d-homo androstane derivatives |
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| Authors: | Evgenija A Djurendi&#x; Marina P Zavi&#x; Marija N Saka
Jano&#x; J anadi Vesna V Koji&#x; Gordana M Bogdanovi&#x; Katarina M Penov Ga&#x;i |
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| Institution: | aDepartment of Chemistry, Faculty of Sciences, University of Novi Sad, Trg Dositeja Obradovića 3, 21000 Novi Sad, Serbia;bOncology Institute of Vojvodina, Institutski put 4, 21204 Sremska Kamenica, Serbia |
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| Abstract: | Starting from 3β-hydroxy-17-oxo-16,17-secoandrost-5-ene-16-nitrile (1), the new 16,17-secoandrostane derivatives 4–9 were synthesized. On the other hand, 3β-hydroxy-17-oxa-d-homoandrost-5-ene-16-one (10) yielded the new d-homo derivatives 12, 13 and 15. In vitro antiproliferative activity of selected compounds against three tumor cell lines (human breast adenocarcinoma ER+, MCF-7, human breast adenocarcinoma ER−, MDA-MB-231, prostate cancer AR−, PC-3, and normal fetal lung fibroblasts, MRC-5) was evaluated. Compounds 3 and 12 showed strong antiproliferative activity against PC-3 cells, the IC50 values being 2 μM and 0.55 μM, respectively. Compounds 6 (10 μM) and 14 (9 μM) showed moderate activity against MDA-MB-231 cells. The synthesized compounds 1–3, 5–8, 10 and 12–15 were not toxic to normal fetal lung fibroblasts cells, MRC-5. |
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| Keywords: | Androstane derivatives 16 17-Secosteroids d-Homosteroids" target="_blank">d-Homosteroids In vitro cytotoxicity |
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