Identification of a Novel Quinoxaline-Isoselenourea Targeting the STAT3 Pathway as a Potential Melanoma Therapeutic.

ABSTRACT: The prognosis for patients with metastatic melanoma remains very poor. Constitutive signal transducer and activator of transcription 3 (STAT3) activation has been correlated to metastasis, poor patient survival, larger tumor size, and acquired resistance against vemurafenib (PLX-4032), suggesting its potential as a molecular target. We recently designed a series of isoseleno- and isothio-urea derivatives of several biologically active heterocyclic scaffolds. The cytotoxic effects of lead isoseleno- and isothio-urea derivatives (compounds 1 and 3) were studied in a panel of five melanoma cell lines, including B-RAFV600E-mutant and wild-type (WT) cells. Compound 1 (IC50 range 0.8⁻3.8 µM) showed lower IC50 values than compound 3 (IC50 range 8.1⁻38.7 µM) and the mutant B-RAF specific inhibitor

SUBMITTER: Alcolea V 

PROVIDER: S-EPMC6386884 | biostudies-literature | 2019 Jan

REPOSITORIES: biostudies-literature