Dipartimento di Scienze Farmaceutiche, Via Belmeloro, 6, I-40126 Bologna, Italy.
Bioorg Med Chem. 2010 May 15;18(10):3543-50. doi: 10.1016/j.bmc.2010.03.069. Epub 2010 Mar 29.
The naturally occurring coumarins and resveratrol, attract great attention due to their wide range of biological properties, including anticancer, antileukemic, antibacterial and anti-inflammatory activities; moreover, their cancer chemopreventive property have been recently emphasized. A novel class of hybrid compounds, obtained by introducing a substituted trans-vinylbenzene moiety on a coumarin backbone, was synthesized and evaluated for the antitumor profile. A number of derivatives showed a good antiproliferative activity, in some cases higher to that of the reference compound resveratrol. The most promising compounds in this series were 14 and 17, endowed with excellent antiproliferative and proapoptotic activities. The present study suggests that the 7-methoxycoumarin nucleus, together with the 3,5-disubstitution pattern of the trans-vinylbenzene moiety, are likely promising structural features to obtain excellent antitumor compounds endowed with a apoptosis-inducing capability.
天然存在的香豆素和白藜芦醇由于其广泛的生物活性而受到极大关注，包括抗癌、抗白血病、抗菌和抗炎活性；此外，它们的癌症化学预防特性最近也受到了重视。通过在香豆素主链上引入取代的反式乙烯基苯部分，合成了一类新型的杂合化合物，并对其抗肿瘤特性进行了评估。许多衍生物表现出良好的增殖抑制活性，在某些情况下比对照化合物白藜芦醇更高。在这个系列中最有前途的化合物是 14 和 17，具有优异的增殖抑制和促凋亡活性。本研究表明，7-甲氧基香豆素核，以及反式乙烯基苯部分的 3,5-取代模式，可能是获得具有凋亡诱导能力的优秀抗肿瘤化合物的有前途的结构特征。
