Peter L. Toogood

Progress toward the development of agents to modulate the cell cycle

With taxanes continuing to prove useful in the clinical treatment of cancer, the next generation of antimitotic agents has entered clinical trials. Other mechanisms awaiting proof-of-concept for the treatment of antiproliferative diseases include inhibition of cyclin-dependent kinases (Cdks). Flavopiridol and UCN-01 are continuing in clinical trials, and newer more selective Cdk inhibitors are now entering clinical evaluation.

Discovery and SAR of benzyl phenyl ethers as inhibitors of bacterial phenylalanyl-tRNA synthetase.

A series of benzyl phenyl ethers (BPEs) is described that displays potent inhibition of bacterial phenylalanyl-tRNA synthetase. The synthesis, SAR, and select ADMET data are provided.

Synthesis of substituted quinazolines

A novel and flexible synthetic route is described for the synthesis of 5,6,8-alkyl-7-methoxy-2-aminoquinazolines using dihydrobenzenes as key intermediates.