32000-30-9Relevant academic research and scientific papers
Hetaryl imidazoles: A novel dual inhibitors of VEGF receptors I and II
Kiselyov, Alexander S.,Semenova, Marina,Semenov, Victor V.
, p. 1440 - 1444 (2006)
A novel potent derivatives of hetaryl imidazoles were described as inhibitors of vascular endothelial growth factor receptor II (VEGFR-2). Several compounds display VEGFR-2 inhibitory activity reaching IC50 100 nM in both enzymatic and cellular assays. The compounds also inhibit the related tyrosine kinase, VEGFR-1. By controlling the substitution pattern on the 5-carboxamido functionality, both dual and specific VEGFR-2 thiazoles were identified.
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.
