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A Concise Total Synthesis of (+)-Neopeltolide

机译:简明全合成(+)-新邻苯二酚

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摘要

(+)-Neopeltolide (1) is a marine macrolide that belongs to the family Neopeltidae, and was isolated from a deep-water sponge collected off the northwest coast of Jamaica by Wright et al . Neopeltolide exhibits highly potent in vitro antiproliferative activity against several cancer cell lines with nanomolar IC_(50) values (IC_(50) = 1.2, 5.1, and 0.56 nmol L~(-1) against the A-549 human lung adenocarcinoma, the NCI-ADR-RES human ovarian sarcoma, and the P388 murine leukemia cells, respectively) as well as potent antifungal activity against pathogenic yeast Candida albicans. Kozmin and co-workers reported that neopeltolide targets cytochrome bc1 complex and may inhibit mitochondrial ATP synthesis. The complex molecular architecture coupled with the intriguing biological activity of 1 have spurred the interest of the synthetic community. A number of total syntheses of 1, including the studies from our research group, have been reported.
机译:(+)-新环内酯(1)是海洋大环内酯类,属于新Neo科,由Wright等人从牙买加西北海岸附近的深水海绵中分离得到。 Neopeltolide对几种癌细胞株具有纳摩尔IC_(50)值(IC_(50)= 1.2、5.1和0.56 nmol L〜(-1)对A-549人肺腺癌NCI的体外增殖能力强-ADR-RES人卵巢肉瘤和P388鼠白血病细胞),以及针对病原酵母白色念珠菌的有效抗真菌活性。 Kozmin及其同事报告说,新pelolide靶向细胞色素bc1复合物,并可能抑制线粒体ATP合成。复杂的分子结构加上令人感兴趣的1的生物学活性激发了合成社区的兴趣。据报道,包括我们研究小组的研究在内的许多1的综合合成。

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