Discovery of CYT997: a structurally novel orally active microtubule targeting agent.
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.
Burns
Christopher J
CJ
Cytopia Research Pty Ltd, Richmond, VIC 3121, Australia.
Harte
Michael F
MF
Bu
Xianyong
X
Fantino
Emmanuelle
E
Joffe
Max
M
Sikanyika
Harrison
H
Su
Stephen
S
Tranberg
C Elisabet
CE
Wilson
Neil
N
Charman
Susan A
SA
Shackleford
David M
DM
Wilks
Andrew F
AF
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
C543949:CYT997; D011725:Pyridines; D011743:Pyrimidines; D050257:Tubulin Modulators