A Novel Sulfonyl-Based Small Molecule Exhibiting Anti-cancer Properties

A Novel Sulfonyl-Based Small Molecule Exhibiting Anti-cancer Properties

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Phenotypic screening is an ideal strategy for the discovery of novel bioactive molecules.Using a customized adifom q red high-throughput screening (HTS) assay employing primary T lymphocytes, we screened a small library of 4,398 compounds with unknown biological function/target to identify compounds eliciting immunomodulatory properties and discovered a sulfonyl-containing hit, we named InhiTinib.This compound inhibited interferon (IFN)-gamma production and proliferation of primary CD3+ T cells without inducing cell death.In contrast, InhiTinib triggered apoptosis in several murine and human cancer cell lines.

Besides, the compound was well tolerated by immunocompetent mice, turbo air m3f24-1 triggered tumor regression in animals with pre-established EL4 T-cell lymphomas, and prolonged the overall survival of mice harboring advanced tumors.Altogether, our data demonstrate the anti-cancer properties of InhiTinib, which can henceforth bridge to wider-scale biochemical and clinical tests following further in-depth pharmacodynamic studies.