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

Authors
Journal
Bioorganic & Medicinal Chemistry Letters
0960-894X
Publisher
Elsevier
Publication Date
Volume
19
Issue
16
Identifiers
DOI: 10.1016/j.bmcl.2009.06.079
Keywords
  • Tubulin Polymerization Inhibitor
  • Microtubule Disruptor
  • Pyrimidine
Disciplines
  • Pharmacology

Abstract

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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