Synthesis and biological evaluation of oxoindolin-3-ylidene ethyl benzothiohydrazides as non-peptide TPO mimics

Peng Cho Tang; He Jun Lu; Yi Qian Chen; Sheng Lan Wang; Hao Zheng; Li Wang

doi:10.1016/j.bmcl.2010.07.040

Synthesis and biological evaluation of oxoindolin-3-ylidene ethyl benzothiohydrazides as non-peptide TPO mimics

Bioorg Med Chem Lett. 2010 Sep 1;20(17):5062-4. doi: 10.1016/j.bmcl.2010.07.040. Epub 2010 Jul 15.

Authors

Peng Cho Tang¹, He Jun Lu, Yi Qian Chen, Sheng Lan Wang, Hao Zheng, Li Wang

Affiliation

¹ Shanghai Hengrui Pharmaceuticals Co., Ltd, Shanghai, China. tangpc@shhrp.com

PMID: 20675136
DOI: 10.1016/j.bmcl.2010.07.040

Abstract

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.

MeSH terms

Cell Line
Drug Evaluation, Preclinical
Humans
Indoles / chemical synthesis*
Indoles / pharmacology*
Molecular Mimicry*
Peptides / chemistry
Receptors, Thrombopoietin / agonists

Substances

Indoles
Peptides
Receptors, Thrombopoietin