A modular synthetic approach toward exhaustively stereodiversified ligand libraries.
A modular synthetic approach toward exhaustively stereodiversified ligand libraries.
复制标题
一种针对彻底立体多样化配体库的模块化合成方法。
作者：
T. M. Gierasch;M. Chytil;M. Didiuk;J. Y. Park;J. Urban;S. Nolan;G. Verdine
[结构]本报告描述了一种合成立体多样性天然产物样文库的模块化方法。单体2和3通过甲硅烷基栓系的烯烃复分解平行偶联以产生顺式烯二醇1的所有16种立体异构体。将所有16种立体异构体掺入具有侧翼肽区段的嵌合体中。这些嵌合体表现出广泛的疏水性，提高了立体化学变化可能被用来调整小分子的药理学特性的可能性。
[structure] This report describes a modular approach to the synthesis of stereodiversified natural product-like libraries. Monomers 2 and 3 were coupled in parallel by silyl-tethered olefin metathesis to generate all 16 stereoisomers of cis-enediols 1. All 16 stereoisomers were incorporated into chimerae having flanking peptidic segments. These chimerae exhibited a broad range of hydrophobicities, raising the possibility that stereochemical variation might be used to tune the pharmacologic properties of small molecules.
影响因子：
56.9
作者：
Mayer, TU;Kapoor, TM;Mitchison, TJ
通讯作者：
Mitchison, TJ