Synthesis and biological evaluation of oxoindolin-3-ylidene ethyl benzothiohydrazides as non-peptide TPO mimics
作者:Peng Cho Tang、He Jun Lu、Yi Qian Chen、Sheng Lan Wang、Hao Zheng、Li Wang
DOI:10.1016/j.bmcl.2010.07.040
日期:2010.9
A novel series of oxoindolin-3-ylidene ethyl benzohydrazides were designed, synthesized, and identified as small molecule agonists of thrombopoietin (TPO) receptor c-mpl. Sulfur–oxygen exchange in oxoindolin-3-ylidene ethyl benzohydrazides was found to improve their agonistic activities. Several oxoindolin-3-ylidene ethyl benzothiohydrazides have been identified as full agonists of c-mpl.
设计,合成和鉴定了一系列新的氧代吲哚-3-亚乙基乙基苯甲酰肼,作为血小板生成素(TPO)受体c-mpl的小分子激动剂。发现氧代吲哚-3-亚乙基乙基苯甲酰肼中的硫-氧交换改善了它们的激动活性。几种氧代吲哚-3-亚乙基乙基苯并硫酰肼已被鉴定为c-mpl的完全激动剂。