Premium
Diarylureas and Diarylamides with Oxazolo[5,4‐ d ]pyrimidine Scaffold as Angiogenesis Inhibitors
Author(s) -
Deng YaHui,
Liu JiPing,
Cheng YiJuan,
Liu Yu,
Sun LiPing
Publication year - 2016
Publication title -
chemistry and biodiversity
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.427
H-Index - 70
eISSN - 1612-1880
pISSN - 1612-1872
DOI - 10.1002/cbdv.201600035
Subject(s) - umbilical vein , chemistry , angiogenesis , in vitro , phosphorylation , pyrimidine , scaffold , kinase , mapk/erk pathway , biochemistry , microbiology and biotechnology , cancer research , biology , biomedical engineering , medicine
A series of oxazolopyrimidine‐based ureas and amides were designed, synthesized, and biologically evaluated for their antiproliferative and antiangiogenic activities. These compounds were identified to exhibit inhibitory activities against human umbilical vein endothelial cells ( HUVEC ) in vitro . Among these compounds, compound 22 effectively inhibited the migration and capillary‐like tube formation of human umbilical vein endothelial cells. It also exhibited a concentration‐dependent inhibition on capillary sprouting from the rat aorta rings. Preliminary mechanistic studies revealed that compound 22 suppressed protein kinases activation, by decreasing PI 3K and ERK 1/2 phosphorylation. These results support the further investigation of this class of compounds as potential anticancer agents.