Bioorganic and Medicinal Chemistry Letters p. 1191 - 1196 (2006)
Update date:2022-08-05
Topics:
Ouyang, Xiaohu
Piatnitski, Evgueni L.
Pattaropong, Vatee
Chen, Xiaoling
He, Hai-Ying
Kiselyov, Alexander S.
Velankar, Avdhoot
Kawakami, Joel
Labelle, Marc
Smith II, Leon
Lohman, Julia
Lee, Sui Ping
Malikzay, Asra
Fleming, James
Gerlak, Jason
Wang, Ying
Rosler, Robin L.
Zhou, Kai
Mitelman, Stan
Camara, Margarita
Surguladze, David
Doody, Jacqueline F.
Tuma, M. Carolina
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 μM. Lead analogs caused mitotic arrest of A431 human epidermoid cells and cells derived from multi-drug resistant tumors (10, EC50 = 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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Doi:10.1002/chem.201502530
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