Chlorinated benzothiadiazines inhibit angiogenesis through suppression of VEGFR2 phosphorylation.

ABSTRACT: Angiogenesis inhibitors are a critical pharmacological tool for the treatment of solid tumors. Suppressing vascular permeability leads to inhibition of tumor growth, invasion, and metastatic potential by blocking the supply of oxygen and nutrients. Disruption of the vascular endothelial growth factor (VEGF) signaling pathway is a validated target for the design of antiangiogenic agents. Several VEGFR2 inhibitors have been clinically approved over the past years. Structural analysis of these clinical VEGFR2 inhibitors highlighted key functional group overlap with the benzothiadiazine core contained in a library of in-house compounds. Herein we ascribe anti-angiogenic activity to a series of chlorinated benzothiadiazines. Selected compounds show significant activity to completely ameliorate

SUBMITTER: Huwaimel BI 

PROVIDER: S-EPMC9888588 | biostudies-literature | 2022 Aug

REPOSITORIES: biostudies-literature