Synthesis and biological evaluation of naphthoquinone analogs as a novel class of proteasome inhibitors.

@article{Lawrence2010SynthesisAB,
  title={Synthesis and biological evaluation of naphthoquinone analogs as a novel class of proteasome inhibitors.},
  author={Harshani R. Lawrence and Aslamuzzaman Kazi and Yunting Luo and Robert Kendig and Yiyu Ge and Sanjula Jain and Kenyon G. Daniel and Daniel N. Santiago and Wayne C. Guida and Sa{\"i}d M. Sebti},
  journal={Bioorganic & medicinal chemistry},
  year={2010},
  volume={18 15},
  pages={5576-92}
}
Screening of the NCI Diversity Set-1 identified PI-083 (NSC-45382) a proteasome inhibitor selective for cancer over normal cells. Focused libraries of novel compounds based on PI-083 chloronaphthoquinone and sulfonamide moieties were synthesized to gain a better understanding of the structure-activity relationship responsible for chymotrypsin-like proteasome inhibitory activity. This led to the demonstration that the chloronaphthoquinone and the sulfonamide moieties are critical for inhibitory… CONTINUE READING