کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1392362 1501131 2014 11 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Design and total synthesis of Mannich derivatives of marine natural product lamellarin D as cytotoxic agents
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Design and total synthesis of Mannich derivatives of marine natural product lamellarin D as cytotoxic agents
چکیده انگلیسی


• Novel design on lamellarin D derivatization.
• Rational attempt for increasing the water-solubility of lamellarin D.
• Multistep synthesis and the strategy of phenol protection.
• Convincing data on Topo I inhibitory and anti-proliferative activities comparing with lamellarin D and lamellarin 501.

Enlightened by the modification route from Camptothecin (CPT) to Topotecan and based on classical drug design theory, a series of Mannich derivatives of lamellarin D were designed and synthesized in 26–27 steps starting from vanillin and isovanilin. All synthesized compounds were then biologically evaluated for their in vitro anti-cancer activities and Topo I inhibitory activities. The results showed that most target compounds exhibited Topo I inhibitory activities in equivalent level with that of lamellarin D. Compound SL-9 exhibited better Topo I inhibitory activity than that of lamellarin D. Compounds SL-2, SL-3, SL-4, SL-5 and SL-11 exhibited better anti-proliferative activity against HT-29 cells than that of lamellarin D.

Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 85, 6 October 2014, Pages 807–817
نویسندگان
, , , , ,