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. 2008 Jan 1;18(1):391-5.
doi: 10.1016/j.bmcl.2007.10.031. Epub 2007 Oct 17.

Design, synthesis, and studies of small molecule STAT3 inhibitors

Deepak Bhasin  1 , Katryna Cisek, Trupti Pandharkar, Nicholas Regan, Chenglong Li, Bulbul Pandit, Jiayuh Lin, Pui-Kai Li
Affiliations

Design, synthesis, and studies of small molecule STAT3 inhibitors

Deepak Bhasin et al. Bioorg Med Chem Lett. .

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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