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扎马内酯和指状内酯：细胞毒性微管组装剂及有前景的抗癌先导化合物。

Zampanolide and dactylolide: cytotoxic tubulin-assembly agents and promising anticancer leads.

作者信息

Chen Qiao-Hong, Kingston David G I

机构信息

Department of Chemistry, California State University, Fresno, 2555 E. San Ramon Avenue, M/S SB70, Fresno, CA 93740, USA.

出版信息

Nat Prod Rep. 2014 Sep;31(9):1202-26. doi: 10.1039/c4np00024b.

DOI:10.1039/c4np00024b
PMID:24945566
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4126874/
Abstract

Zampanolide is a marine natural macrolide and a recent addition to the family of microtubule-stabilizing cytotoxic agents. Zampanolide exhibits unique effects on tubulin assembly and is more potent than paclitaxel against several multi-drug resistant cancer cell lines. A high-resolution crystal structure of αβ-tubulin in complex with zampanolide explains how taxane-site microtubule-stabilizing agents promote microtubule assemble and stability. This review provides an overview of current developments of zampanolide and its related but less potent analogue dactylolide, covering their natural sources and isolation, structure and conformation, cytotoxic potential, structure-activity studies, mechanism of action, and syntheses.

摘要

扎马普隆是一种海洋天然大环内酯类化合物，是微管稳定细胞毒性药物家族中的新成员。扎马普隆对微管蛋白组装具有独特作用，在几种多药耐药癌细胞系中比紫杉醇更具活性。αβ-微管蛋白与扎马普隆复合物的高分辨率晶体结构解释了紫杉烷位点微管稳定剂如何促进微管组装和稳定性。本综述概述了扎马普隆及其相关但活性较低的类似物达克替洛内酯的当前研究进展，涵盖其天然来源与分离、结构与构象、细胞毒性潜力、构效关系研究、作用机制以及合成方法。

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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d6e7/4326965/79c1ef4e0dcc/c4np00024b-p2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d6e7/4326965/1aca37f51177/c4np00024b-s30.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d6e7/4326965/e0f2d641ab9a/c4np00024b-s31.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d6e7/4326965/15c99d7ec50f/c4np00024b-s32.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d6e7/4326965/e2094bb9f9e6/c4np00024b-s33.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d6e7/4326965/1a767405adfb/c4np00024b-s37.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d6e7/4326965/3db920c77c11/c4np00024b-s39.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d6e7/4326965/b1cb3dca12b6/c4np00024b-s40.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d6e7/4326965/6421c918d115/c4np00024b-s42.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d6e7/4326965/bc62325bca07/c4np00024b-s43.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d6e7/4326965/1853ff79ab72/c4np00024b-s44.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d6e7/4326965/f6df90591799/c4np00024b-p1.jpg
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