bp-1-102 and Neoplasms

STAT3 plays a vital role in maintaining the self-renewal of tumor stem cells. BBI608, a small molecule identified by its ability to inhibit gene transcription driven by STAT3 and cancer stemness properties, can inhibit stemness gene expression and kill stemness-high cancer cells isolated from a variety of cancer types. In order to improve the pharmacokinetic properties of BBI608 and the antitumor activity, a series of BBI608 derivatives were designed and synthesized here. Most of these compounds were more potent than BBI608 on HepG2 cells, compound LD-8 had the most potent inhibitory activity among them and was 5.4-fold more potent than BBI608 (IC

Topics: Antineoplastic Agents; Benzofurans; Cell Proliferation; Drug Design; Drug Screening Assays, Antitumor; Hep G2 Cells; Humans; Molecular Docking Simulation; Naphthoquinones; Neoplasms; Neoplastic Stem Cells; STAT3 Transcription Factor