کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2027918 1542714 2015 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis and biological evaluation of novel sarsasapogenin derivatives as potential anti-tumor agents
ترجمه فارسی عنوان
سنتز و بررسی بیولوژیکی مشتقات ساراساپاپژنین جدید به عنوان عوامل بالقوه ضد تومور
کلمات کلیدی
اسپیرستان، ساراساپوژنین، مشتقات آمینوفورواست 26، مشتقات 3-آمین اسپروئین، فعالیت ضد تومور
موضوعات مرتبط
علوم زیستی و بیوفناوری بیوشیمی، ژنتیک و زیست شناسی مولکولی زیست شیمی
چکیده انگلیسی


• A series of nitrogen-containing sarsasapogenin derivatives has been synthesized.
• A piperazinyl group at C-3 increased the cytotoxic activity.
• Furostanic C-26 nitrogenated compounds showed anti-proliferative activity.
• Some compounds displayed excellent selective cytotoxicity compared with 5-FU.

Based on the fact that timosaponin A-III (TA-III) exhibits potent cytotoxic effects and has been considered as a potential anti-tumor agent, a range of novel sarsasapogenin derivatives 1, 2a–2g, 3, 4, 5, 6a–6g have been synthesized by a simple and facile synthetic route. The in vitro cytotoxic activity of these synthetic compounds has been evaluated against ten human cancer cell lines. The pharmacological results showed that most of the sarsasapogenin derivatives displayed excellent selective cytotoxicity toward the cancer cell lines. An amino group at C-3 or C-26 position of the sapogenin had a profound influence on the cytotoxic activity. In particular, compound 6c exhibited significantly inhibitory activity against A375-S2 (IC50 = 0.56 μM) and HT1080 (IC50 = 0.72 μM) cells. However, introducing a bromo or morpholinyl substituent at the C-3 and C-26 position of the sapogenin generally rendered it inactive against the human cancer cell lines. This research provides a theoretical reference for the exploration of new anti-tumor drugs.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Steroids - Volume 93, January 2015, Pages 25–31
نویسندگان
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