全合成设计的微管稳定剂抗癌药物紫杉醇、discodermolide 和 dictyostatin 杂交文库。
Total synthesis of a library of designed hybrids of the microtubule-stabilising anticancer agents taxol, discodermolide and dictyostatin.
机构信息
University Chemical Laboratory, Lensfield Road, Cambridge, UK, CB2 1EW.
出版信息
Chem Commun (Camb). 2010 Jan 14;46(2):261-3. doi: 10.1039/b921237j. Epub 2009 Nov 24.
DOI:10.1039/b921237j
PMID:20024345
Abstract
A hybrid library of the marine natural products dictyostatin and discodermolide, incorporating the taxol or taxotere side chains, were synthesised; preliminary biological evaluation in the PANC-1 cancer cell line revealed significant antiproliferative activity, demonstrating that a macrolide scaffold is an effective surrogate for the baccatin core of taxol.
摘要
混合文库的海洋天然产物海鞘素和 discodermolide ，纳入紫杉醇或多烯紫杉醇侧链，被合成 ；初步的生物评价在 PANC-1 癌细胞系中显示出显著的抗增殖活性，表明大环内酯支架是紫杉醇的 baccatin 核心的有效替代物。
Zotero 插件