Identification of a novel chalcone derivative that inhibits Notch signaling in T-cell acute lymphoblastic leukemia.

ABSTRACT: Notch signaling is considered a rational target in the therapy of several cancers, particularly those harbouring Notch gain of function mutations, including T-cell acute lymphoblastic leukemia (T-ALL). Although currently available Notch-blocking agents are showing anti-tumor activity in preclinical studies, they are not effective in all the patients and often cause severe side-effects, limiting their widespread therapeutic use. Here, by functional and biological analysis of the most representative molecules of an in house library of natural products, we have designed and synthetized the chalcone-derivative 8 possessing Notch inhibitory activity at low micro molar concentration in T-ALL cell lines. Structure-activity relationships were afforded for the chalcone scaffold. Short term treatmen

SUBMITTER: Mori M 

PROVIDER: S-EPMC5438367 | biostudies-literature | 2017 May

REPOSITORIES: biostudies-literature