Synthesis and biological evaluation of oxoindolin-3-ylidene ethyl benzothiohydrazides as non-peptide TPO mimics.
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.
Tang
Peng Cho
PC
Shanghai Hengrui Pharmaceuticals Co., Ltd, Shanghai, China. tangpc@shhrp.com
Lu
He Jun
HJ
Chen
Yi Qian
YQ
Wang
Sheng Lan
SL
Zheng
Hao
H
Wang
Li
L
D002460:Cell Line; D004353:Drug Evaluation, Preclinical; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D018716:Molecular Mimicry; D010455:Peptides / Q000737:chemistry; D053628:Receptors, Thrombopoietin / Q000819:agonists
D007211:Indoles; D010455:Peptides; D053628:Receptors, Thrombopoietin