α,β-Unsaturated carbonyl system of chalcone-based derivatives is responsible for broad inhibition of proteasomal activity and preferential killing of human papilloma virus (HPV) positive cervical cancer cells.

@article{Bazzaro2011UnsaturatedCS,
  title={α,β-Unsaturated carbonyl system of chalcone-based derivatives is responsible for broad inhibition of proteasomal activity and preferential killing of human papilloma virus (HPV) positive cervical cancer cells.},
  author={Martina Bazzaro and Ravi Kumar Anchoori and Mohana Krishna Reddy Mudiam and Olga A. Issaenko and Srinivas K. Kumar and Balasubramanyam Karanam and Zhenhua Lin and Rachel Isaksson Vogel and Riccardo Gavioli and Federica Destro and Valeria Ferretti and Richard B. S. Roden and Saeed R Khan},
  journal={Journal of medicinal chemistry},
  year={2011},
  volume={54 2},
  pages={449-56}
}
Proteasome inhibitors have potential for the treatment of cervical cancer. We describe the synthesis and biological characterization of a new series of 1,3-diphenylpropen-1-one (chalcone) based derivatives lacking the boronic acid moieties of the previously reported chalcone-based proteasome inhibitor 3,5-bis(4-boronic acid benzylidene)-1-methylpiperidin-4-one and bearing a variety of amino acid substitutions on the amino group of the 4-piperidone. Our lead compound 2 (RA-1) inhibits… CONTINUE READING