Discovery of CYT997: a structurally novel orally active microtubule targeting agent

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

doi:10.1016/j.bmcl.2009.06.079

Discovery of CYT997: a structurally novel orally active microtubule targeting agent

Bioorg Med Chem Lett. 2009 Aug 15;19(16):4639-42. doi: 10.1016/j.bmcl.2009.06.079. Epub 2009 Jun 25.

Authors

Christopher J Burns¹, 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

Affiliation

¹ Cytopia Research Pty Ltd, Richmond, VIC 3121, Australia.

PMID: 19616947
DOI: 10.1016/j.bmcl.2009.06.079

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.

MeSH terms

Administration, Oral
Animals
Cell Line, Tumor
Drug Discovery
Humans
Microtubules / chemistry*
Microtubules / metabolism
Pyridines / administration & dosage
Pyridines / chemistry*
Pyridines / pharmacokinetics
Pyrimidines / administration & dosage
Pyrimidines / chemistry*
Pyrimidines / pharmacokinetics
Rats
Structure-Activity Relationship
Tubulin Modulators / administration & dosage
Tubulin Modulators / chemistry*
Tubulin Modulators / pharmacokinetics

Substances

CYT997
Pyridines
Pyrimidines
Tubulin Modulators