Literature DB >> 18006313

Design, synthesis, and studies of small molecule STAT3 inhibitors.

Deepak Bhasin1, Katryna Cisek, Trupti Pandharkar, Nicholas Regan, Chenglong Li, Bulbul Pandit, Jiayuh Lin, Pui-Kai Li.   

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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Year:  2007        PMID: 18006313     DOI: 10.1016/j.bmcl.2007.10.031

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  29 in total

Review 1.  Targeting STAT3 in cancer: how successful are we?

Authors:  Peibin Yue; James Turkson
Journal:  Expert Opin Investig Drugs       Date:  2009-01       Impact factor: 6.206

2.  Fragment-based drug design and drug repositioning using multiple ligand simultaneous docking (MLSD): identifying celecoxib and template compounds as novel inhibitors of signal transducer and activator of transcription 3 (STAT3).

Authors:  Huameng Li; Aiguo Liu; Zhenjiang Zhao; Yufang Xu; Jiayuh Lin; David Jou; Chenglong Li
Journal:  J Med Chem       Date:  2011-07-08       Impact factor: 7.446

3.  Radiation induces an inflammatory response that results in STAT3-dependent changes in cellular plasticity and radioresistance of breast cancer stem-like cells.

Authors:  Kimberly M Arnold; Lynn M Opdenaker; Nicole J Flynn; Daniel Kwesi Appeah; Jennifer Sims-Mourtada
Journal:  Int J Radiat Biol       Date:  2020-01-06       Impact factor: 2.694

Review 4.  A complex task? Direct modulation of transcription factors with small molecules.

Authors:  Angela N Koehler
Journal:  Curr Opin Chem Biol       Date:  2010-04-13       Impact factor: 8.822

Review 5.  Targeting SH2 domains in breast cancer.

Authors:  Pietro Morlacchi; Fredika M Robertson; Jim Klostergaard; John S McMurray
Journal:  Future Med Chem       Date:  2014       Impact factor: 3.808

Review 6.  STAT3 regulation of glioblastoma pathogenesis.

Authors:  Núria de la Iglesia; Sidharth V Puram; Azad Bonni
Journal:  Curr Mol Med       Date:  2009-06       Impact factor: 2.222

7.  Dual-inhibitors of STAT5 and STAT3: studies from molecular docking and molecular dynamics simulations.

Authors:  Shengjuan Shao; Rilei Yu; Yanqing Yu; Yanni Li
Journal:  J Mol Model       Date:  2014-08-07       Impact factor: 1.810

8.  Lack of toxicity of a STAT3 decoy oligonucleotide.

Authors:  Malabika Sen; Patricia J Tosca; Christa Zwayer; Michael J Ryan; Jerry D Johnson; Katherine A B Knostman; Patricia C Giclas; James O Peggins; Joseph E Tomaszewski; Timothy P McMurray; Changyou Li; Michael S Leibowitz; Robert L Ferris; William E Gooding; Sufi M Thomas; Daniel E Johnson; Jennifer R Grandis
Journal:  Cancer Chemother Pharmacol       Date:  2008-09-03       Impact factor: 3.333

9.  A novel small-molecule disrupts Stat3 SH2 domain-phosphotyrosine interactions and Stat3-dependent tumor processes.

Authors:  Xiaolei Zhang; Peibin Yue; Steven Fletcher; Wei Zhao; Patrick T Gunning; James Turkson
Journal:  Biochem Pharmacol       Date:  2010-01-11       Impact factor: 5.858

10.  Characterization of STAT3 activation and expression in canine and human osteosarcoma.

Authors:  Stacey L Fossey; Albert T Liao; Jennifer K McCleese; Misty D Bear; Jiayuh Lin; Pui-Kai Li; William C Kisseberth; Cheryl A London
Journal:  BMC Cancer       Date:  2009-03-10       Impact factor: 4.430

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