Design, synthesis, and studies of small molecule STAT3 inhibitors |
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| Authors: | Bhasin Deepak Cisek Katryna Pandharkar Trupti Regan Nicholas Li Chenglong Pandit Bulbul Lin Jiayuh Li Pui-Kai |
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| Institution: | Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 338 Parks Hall, 500 West 12th Avenue, Columbus, OH 43210, USA. |
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| 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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