Discovery of 2-Pyrazolines That Inhibit the Phosphorylation of STAT3 as Nanomolar Cytotoxic Agents.

ABSTRACT: STAT3 has emerged as a validated target in cancer, being functionally associated with breast cancer (BC) development, growth, resistance to chemotherapy, metastasis, and evasion of immune surveillance. Previously, a series of compounds consisting of imidazo[1,2-a]pyridine tethered 2-pyrazolines (referred to as ITPs) were developed that inhibit STAT3 phosphorylation in estrogen receptor-positive (ER+) BC cells. Herein, a new library of derivatives consisting of imidazo[1,2-a]pyridine clubbed 2-pyrazolines 2(a-o) and its amide derivatives 3(a-af) have been synthesized. Among these derivatives, 3n and 3p displayed efficacy to reduce ER+ BC cell viability, with IC₅₀ values of 55 and 15 nM, respectively. Molecular

SUBMITTER: Siddappa TP 

PROVIDER: S-EPMC11740381 | biostudies-literature | 2025 Jan

REPOSITORIES: biostudies-literature