title: Discovery of CYT997: a structurally novel orally active microtubule targeting agent.
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.
authors.affiliation: Cytopia Research Pty Ltd, Richmond, VIC 3121, Australia.
authors.forename: Christopher J
authors.initials: CJ
authors.lastname: Burns
authors.forename: Michael F
authors.initials: MF
authors.lastname: Harte
authors.forename: Xianyong
authors.initials: X
authors.lastname: Bu
authors.forename: Emmanuelle
authors.initials: E
authors.lastname: Fantino
authors.forename: Max
authors.initials: M
authors.lastname: Joffe
authors.forename: Harrison
authors.initials: H
authors.lastname: Sikanyika
authors.forename: Stephen
authors.initials: S
authors.lastname: Su
authors.forename: C Elisabet
authors.initials: CE
authors.lastname: Tranberg
authors.forename: Neil
authors.initials: N
authors.lastname: Wilson
authors.forename: Susan A
authors.initials: SA
authors.lastname: Charman
authors.forename: David M
authors.initials: DM
authors.lastname: Shackleford
authors.forename: Andrew F
authors.initials: AF
authors.lastname: Wilks
mesh_terms: D000284:Administration, Oral; D000818:Animals; D045744:Cell Line, Tumor; D055808:Drug Discovery; D006801:Humans; D008870:Microtubules / Q000737:chemistry* / Q000378:metabolism; D011725:Pyridines / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D011743:Pyrimidines / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D013329:Structure-Activity Relationship; D050257:Tubulin Modulators / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics
chemical_list: C543949:CYT997; D011725:Pyridines; D011743:Pyrimidines; D050257:Tubulin Modulators