Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors.

  title={Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors.},
  author={Noel D D'Angelo and Tae-Seong Kim and Kristin L. Andrews and Shon K Booker and Sean Caenepeel and Kui Chen and Derin C. D'Amico and Dan Freeman and Jian Jiang and Longbin Liu and John D McCarter and Tisha San Miguel and Erin L Mullady and Michael Schrag and R. Venkata Subramanian and Jin Tang and Robert C. Wahl and Ling Wang and Douglas A. Whittington and Tian Wu and Ning Xi and Yang Xu and Peter S. Yakowec and Kevin Wenjun Yang and Leeanne P Zalameda and Nancy Y Zhang and Paul E. Hughes and Mark H. Norman},
  journal={Journal of medicinal chemistry},
  volume={54 6},
Phosphoinositide 3-kinase α (PI3Kα) is a lipid kinase that plays a key regulatory role in several cellular processes. The mutation or amplification of this kinase in humans has been implicated in the growth of multiple tumor types. Consequently, PI3Kα has become a target of intense research for drug discovery. Our studies began with the identification of benzothiazole compound 1 from a high throughput screen. Extensive SAR studies led to the discovery of sulfonamide 45 as an early lead, based… CONTINUE READING


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