2-Sulfonylpyrimidines: Mild alkylating agents with anticancer activity toward p53-compromised cells.

@article{Bauer20162SulfonylpyrimidinesMA,
  title={2-Sulfonylpyrimidines: Mild alkylating agents with anticancer activity toward p53-compromised cells.},
  author={Matthias R. Bauer and Andreas C. Joerger and A. R. Fersht},
  journal={Proceedings of the National Academy of Sciences of the United States of America},
  year={2016},
  volume={113 36},
  pages={E5271-80}
}
The tumor suppressor p53 has the most frequently mutated gene in human cancers. Many of p53's oncogenic mutants are just destabilized and rapidly aggregate, and are targets for stabilization by drugs. We found certain 2-sulfonylpyrimidines, including one named PK11007, to be mild thiol alkylators with anticancer activity in several cell lines, especially those with mutationally compromised p53. PK11007 acted by two routes: p53 dependent and p53 independent. PK11007 stabilized p53 in vitro via… CONTINUE READING
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