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Discovery of CYT997: a structurally novel orally active microtubule targeting agent
Authors:Christopher J Burns  Michael F Harte  Xianyong Bu  Emmanuelle Fantino  Max Joffe  Harrison Sikanyika  Stephen Su  C Elisabet Tranberg  Neil Wilson  Susan A Charman  David M Shackleford  Andrew F Wilks
Institution:1. Cytopia Research Pty Ltd, 576 Swan St, Richmond, VIC 3121, Australia;2. Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, VIC 3052, Australia
Abstract:CYT997 was discovered as a potent tubulin polymerization inhibitor possessing potent cytotoxic activity against a range of cancer cells. Details of SAR studies, pharmacokinetic investigations and synthesis of compounds leading to the discovery of CYT997 are reported.
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