کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1392362 | 1501131 | 2014 | 11 صفحه PDF | دانلود رایگان |
• 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.
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Journal: European Journal of Medicinal Chemistry - Volume 85, 6 October 2014, Pages 807–817