2. Academic Validation
  3. Oxadiazole derivatives as a novel class of antimitotic agents: Synthesis, inhibition of tubulin polymerization, and activity in tumor cell lines

Oxadiazole derivatives as a novel class of antimitotic agents: Synthesis, inhibition of tubulin polymerization, and activity in tumor cell lines

  • Bioorg Med Chem Lett. 2006 Mar 1;16(5):1191-6. doi: 10.1016/j.bmcl.2005.11.094.
Xiaohu Ouyang 1,  Evgueni L Piatnitski,  Vatee Pattaropong,  Xiaoling Chen,  Hai-Ying He,  Alexander S Kiselyov,  Avdhoot Velankar,  Joel Kawakami,  Marc Labelle,  Leon Smith 2nd,  Julia Lohman,  Sui Ping Lee,  Asra Malikzay,  James Fleming,  Jason Gerlak,  Ying Wang,  Robin L Rosler,  Kai Zhou,  Stan Mitelman,  Margarita Camara,  David Surguladze,  Jacqueline F Doody,  M Carolina Tuma
Affiliations

Affiliation

  • 1 Department of Chemistry, ImClone Systems Incorporated, 180 Varick Street, New York, NY 10014, USA. shawn_ouyang@yahoo.com
PMID: 16377187 DOI: 10.1016/j.bmcl.2005.11.094
Abstract

Oxadiazole derivatives were synthesized and evaluated for their ability to inhibit tubulin polymerization and to cause mitotic arrest in tumor cells. The most potent compounds inhibited tubulin polymerization at concentrations below 1 microM. Lead analogs caused mitotic arrest of A431 human epidermoid cells and cells derived from multi-drug resistant tumors (10, EC(50)=7.8 nM). Competition for the colchicine binding site and pharmacokinetic properties of selected potent compounds were also investigated and are reported herein, along with structure-activity relationships for this novel series of antimitotic agents.

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