Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugs.

  title={Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugs.},
  author={William H. Bisson and Anton V. Cheltsov and Nathalie Bruey-Sedano and Bing Lin and Joy Chen and Natalie E Goldberger and Lester T. May and Arthur Christopoulos and James T Dalton and Patrick M. Sexton and X-k Zhang and Ruben Abagyan},
  journal={Proceedings of the National Academy of Sciences of the United States of America},
  volume={104 29},
Finding good drug leads de novo from large chemical libraries, real or virtual, is not an easy task. High-throughput screening is often plagued by low hit rates and many leads that are toxic or exhibit poor bioavailability. Exploiting the secondary activity of marketed drugs, on the other hand, may help in generating drug leads that can be optimized for the observed side-effect target, while maintaining acceptable bioavailability and toxicity profiles. Here, we describe an efficient… CONTINUE READING


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