Synthesis and biological evaluation of Apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.

@article{Wei2010SynthesisAB,
  title={Synthesis and biological evaluation of Apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.},
  author={Jun Koh Wei and Shinichi Kitada and John L. Stebbins and W. Placzek and Dayong Zhai and Bainan Wu and Michele F. Rega and Ziming Zhang and Jason F Cellitti and Li Yang and Russell Dahl and John C. Reed and Maurizio Pellecchia},
  journal={Journal of medicinal chemistry},
  year={2010},
  volume={53 22},
  pages={8000-11}
}
Overexpression of antiapoptotic Bcl-2 family proteins is commonly related with tumor maintenance, progression, and chemoresistance. Inhibition of these antiapoptotic proteins is an attractive approach for cancer therapy. Guided by nuclear magnetic resonance (NMR) binding assays, a series of 5,5' substituted compound 6a (Apogossypolone) derivatives was synthesized and identified pan-active antagonists of antiapoptotic Bcl-2 family proteins, with binding potency in the low micromolar to nanomolar… CONTINUE READING
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Gossypolone for the treatment of cancer

  • M. R. Flack, R. Knazek, M. Reidenberg
  • U.S. Patent 40862
  • 2009

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