Kim Eun Jin, Ko Soo Y
Department of Chemistry and Division of Molecular Life Sciences, Ewha Womans University, Seoul 120-750, Korea.
Bioorg Med Chem. 2005 Jun 2;13(12):4103-12. doi: 10.1016/j.bmc.2005.03.037. Epub 2005 Apr 25.
A series of arylidene-substituted gelastatin analogues were synthesized in a divergent manner. Each analogue was obtained as a mixture of isomers. Calculation methods were devised to deduce the MMP-2 inhibitory activity of each isomer from the activity of an isomeric mixture and its composition. This protocol is suitable for rapidly generating a variety of arylidene-substituted gelastatin analogues and screening them for highly active inhibitors.
以发散方式合成了一系列亚芳基取代的明胶酶抑制素类似物。每个类似物均以异构体混合物的形式获得。设计了计算方法，以便根据异构体混合物的活性及其组成来推断每种异构体的基质金属蛋白酶-2抑制活性。该方案适用于快速生成多种亚芳基取代的明胶酶抑制素类似物，并筛选出高活性抑制剂。
