[1]田丹碧,章靖,祝艳琳,等.紫杉醇构效关系及类似物生物活性的研究进展[J].南京师范大学学报(工程技术版),2007,07(04):048-54.
 Tian Danbi,Zhang Jing,Zhu yanlin,et al.Advances in Structure-Activity Relationship of Paclitaxel and Bioactivity of Analogues[J].Journal of Nanjing Normal University(Engineering and Technology),2007,07(04):048-54.
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紫杉醇构效关系及类似物生物活性的研究进展
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南京师范大学学报(工程技术版)[ISSN:1006-6977/CN:61-1281/TN]

卷:
07卷
期数:
2007年04期
页码:
048-54
栏目:
出版日期:
2007-12-30

文章信息/Info

Title:
Advances in Structure-Activity Relationship of Paclitaxel and Bioactivity of Analogues
作者:
田丹碧;章靖;祝艳琳;李万博;陈禹;
南京工业大学理学院, 江苏南京210009
Author(s):
Tian DanbiZhang JingZhu yanlinLi WanboChen Yu
College of Science,Nanjing University of Technology,Nanjing 210009,China
关键词:
紫杉醇 构效关系 生物活性
Keywords:
paclitax el structure-ac tiv ity relationsh ip b ioactiv ity
分类号:
R914
摘要:
紫杉醇是当今最有效的抗癌药物之一.它的作用机理独特,通过诱导和促进微管蛋白聚合形成稳定结构,从而抑制微管解聚.对紫杉醇的构效与活性之间的关系以及近十年来紫杉醇类似物研究进展进行了比较详尽的阐述,包括以下几个方面:C2位苯甲酰基、C4位乙酰基、D环、C13侧链、C2与C3′成环、C4与C3′成环以及其它位基团对紫杉醇生物活性的影响.从紫杉醇的构效关系看,C1、C7、C9和C10位基团对它的生物活性并无太大的影响,但是C2、C4位的基团以及D环和C13位的侧链对紫杉醇的生物活性影响重大.
Abstract:
Paclitax el is considered one of them ost prom ising antitum or druggery. It po ssesses a un iquem echanism o f action as promo ters of tubulin aseemb ly and inhibitors of m icro tubu le disassem bly. W em ake a com prehensive summ ary o f the re lationship between the struc ture-effect of paclitaxe l and its b io activ ity and stud ies of paclitax el. s analogues. Topics discussed include: e ffects o f C2-benzoy,l C4-aceta te, D-r ing, C13 s ide chain, C2- C3c- linked m acro cyc lic, C4- C3c- linked m acrocyc lic and o ther groups on bioactiv ity of paclitax e.l From struc ture-effect re lationsh ip of pac litaxe,l groups o f C1, C7, C9 and C10 have weake r effect on its bioactiv ity, wh ile C2-benzoy ,l C4-aceta te, Dr ing and C13 side cha in have stronger effect on it

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备注/Memo

备注/Memo:
作者简介: 田丹碧( 1962-) , 女, 教授, 博士, 主要从事现代分析方面的教学与研究. E-m ail: t iand anbi@126. com
更新日期/Last Update: 2013-04-29