830334-33-3Relevant academic research and scientific papers
Oxadiazole derivatives as a novel class of antimitotic agents: Synthesis, inhibition of tubulin polymerization, and activity in tumor cell lines
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
, p. 1191 - 1196 (2007/10/03)
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.
Synthesis and structure-activity relationships of 1,2,4-triazoles as a novel class of potent tubulin polymerization inhibitors
Ouyang, Xiaohu,Chen, Xiaoling,Piatnitski, Evgueni L.,Kiselyov, Alexander S.,He, Hai-Ying,Mao, Yunyu,Pattaropong, Vatee,Yu, Yang,Kim, Ki H.,Kincaid, John,Smith II, Leon,Wong, Wai C.,Lee, Sui Ping,Milligan, Daniel L.,Malikzay, Asra,Fleming, James,Gerlak, Jason,Deevi, Dhanvanthri,Doody, Jacqueline F.,Chiang, Hui-Hsien,Patel, Sheetal N.,Wang, Ying,Rolser, Robin L.,Kussie, Paul,Labelle, Marc,Tuma, M. Carolina
, p. 5154 - 5159 (2007/10/03)
A novel triazole-containing chemical series was shown to inhibit tubulin polymerization and cause cell cycle arrest in A431 cancer cells with EC 50 values in the single digit nanomolar range. Binding experiments demonstrated that representative
