Synthesis and evaluation of aminothiazole derivatives as hedgehog pathway inhibitors.

Synthesis and evaluation of aminothiazole derivatives as hedgehog pathway inhibitors.
Chem Biodivers. 2019 Oct 14;:
Authors: Sun C, Zhang Y, Lin L, Liu S, Wang R, Zang W, Meng W, Chen X
Abstract
A series of aminothiazole derivatives bearing the benzimidazole moiety were synthesized, and evaluated in Gli luciferase reporter assays. Lead optimization led to the discovery of potent hedgehog pathway antagonist 18, with IC 50 values in nanomolar range. The molecular basis ascribed to hindering sonic hedgehog-driven Smoothened (Smo) localization within the primary cilium (PC). Moreover, compound 18 inhibited Gli1 mRNA expression in mutant Smo cell line and displayed moderate cytotoxicity against DAOY cancer cell.
PMID: 31609078 [PubMed - as supplied by publisher]

Source: Chemistry and Biodiversity - October 13, 2019 Category: Biochemistry Authors: Sun C, Zhang Y, Lin L, Liu S, Wang R, Zang W, Meng W, Chen X Tags: Chem Biodivers Source Type: research