2. Academic Validation
  3. Design, synthesis, and studies of small molecule STAT3 inhibitors

Design, synthesis, and studies of small molecule STAT3 inhibitors

  • Bioorg Med Chem Lett. 2008 Jan 1;18(1):391-5. doi: 10.1016/j.bmcl.2007.10.031.
Deepak Bhasin 1,  Katryna Cisek,  Trupti Pandharkar,  Nicholas Regan,  Chenglong Li,  Bulbul Pandit,  Jiayuh Lin,  Pui-Kai Li
Affiliations

Affiliation

  • 1 Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 338 Parks Hall, 500 West 12th Avenue, Columbus, OH 43210, USA.
PMID: 18006313 DOI: 10.1016/j.bmcl.2007.10.031
Abstract

A series of small molecule STAT3 inhibitors originally derived from our lead compound STA 21 were synthesized and evaluated. The most potent compound in this series, compound 1, exhibited the same anti-proliferative activities as STA 21 against prostate Cancer cell lines that express constitutively active STAT3. Molecular docking showed compound 1 bound to the STAT3beta SH2 domain in a similar manner as STA 21.

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