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首页> 外文期刊>RSC Advances >Synthesis and anticancer studies of Michael adducts and Heck arylation products of sesquiterpene lactones, zaluzanin D and zaluzanin C from Vernonia arborea
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Synthesis and anticancer studies of Michael adducts and Heck arylation products of sesquiterpene lactones, zaluzanin D and zaluzanin C from Vernonia arborea

机译：倍半萜萜内酯，扎鲁赞宁D和扎鲁赞宁C的迈克尔加合物和Heck芳基化产物的合成和抗癌研究

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摘要

Sesquiterpene lactones containing α-methylene-γ-lactones, zaluzanin D 1 and zaluzanin C 2 were isolated from the leaves of Vernonia arborea . Several diverse Michael adducts ( 3–22 ) and Heck arylation analogs ( 23–34 ) of 1 have been synthesized by reacting with various amines and aryl iodides, respectively and were assayed for their in vitro anticancer activities against human breast cancer cell lines MCF7 and MDA-MB-231. Among all the synthesized analogs, Michael adducts 9 and 10 showed better anticancer activities as compared to 1 . However, among these compounds, only 10 has minimal cytotoxic effect on normal breast epithelial MCF10A cells. Our detailed mechanistic studies reveal that compounds 9 and 10 execute their antiproliferative activity through induction of apoptosis and thereby inhibit the cancer cells proliferation and compound 10 could be a lead compound for designing potential anti-cancer compound.
机译：从树莓（Vernonia arborea）的叶片中分离出含有α-亚甲基-γ-内酯，zaluzanin D 1和zaluzanin C 2的倍半萜内酯。分别通过与各种胺和碘代芳烃反应合成了1的几种不同的迈克尔加合物（3–22）和Heck芳基化类似物（23–34），并对其在体外对人乳腺癌细胞MCF7和MDA-MB-231。在所有合成的类似物中，迈克尔加合物9和10与1相比显示出更好的抗癌活性。但是，在这些化合物中，只有10种对正常乳腺上皮MCF10A细胞具有最小的细胞毒性作用。我们详细的机理研究表明，化合物9和10通过诱导细胞凋亡来执行其抗增殖活性，从而抑制癌细胞的增殖，化合物10可能是设计潜在抗癌化合物的先导化合物。

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