放线菌素D新类似物的合成与生物学评价
Synthesis and biological evaluation of novel analogues of dictyostatin.
作者信息
Paterson Ian, Gardner Nicola M, Poullennec Karine G, Wright Amy E
机构信息
University Chemical Laboratory, Lensfield Road, Cambridge CB2 1EW, UK.
出版信息
Bioorg Med Chem Lett. 2007 May 1;17(9):2443-7. doi: 10.1016/j.bmcl.2007.02.031. Epub 2007 Feb 14.
PMID:17336522
Abstract
Novel analogues of the microtubule-stabilising agent dictyostatin were designed using existing SAR information from the structurally related discodermolide, synthesised by a late-stage diversification strategy and evaluated in vitro for growth inhibition against a range of human cancer cell lines, including those known to exhibit Taxol-resistance (AsPC-1, DLD-1, PANC-1, NCI/ADR).
摘要
利用来自结构相关的盘状内酯的现有构效关系信息，设计了微管稳定剂双鞭甲藻素的新型类似物，通过后期多样化策略进行合成，并在体外评估其对一系列人类癌细胞系的生长抑制作用，包括那些已知对紫杉醇耐药的细胞系（AsPC-1、DLD-1、PANC-1、NCI/ADR）。
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