@article{oai:tsukuba.repo.nii.ac.jp:00054331, author = {吉田, 将人 and YOSHIDA, Masahito}, issue = {10}, journal = {Chemical & pharmaceutical bulletin}, month = {Oct}, note = {The combinatorial synthesis and biological evaluation of destruxins are described herein. First, the total synthesis of destruxin E was achieved, and its absolute configuration was successfully determined to be (S). In addition, the preparation of a combinatorial library based on the structure of destruxins was carried out by the split-and-pool method. Biological evaluation of the resulting analogs against osteoclast-like multinuclear cells (OCLs) revealed that the N-methyl-alanine residue was crucial to inducing morphological changes in OCLs. In particular, functionalization at the β-position of the proline (Pro) residue was found to be tolerant of the desired biological activity of destruxin E, suggesting that the β-position of the Pro residue should be a promising site for the introduction of a chemical tag toward the preparation of a molecular probe.}, pages = {1023--1029}, title = {Combinatorial Synthesis and Biological Evaluation of Destruxins}, volume = {67}, year = {2019}, yomi = {ヨシダ, マサヒト} }