214758-59-5Relevant academic research and scientific papers
Discovery of a new class of glucosylceramide synthase inhibitors
Koltun, Elena,Richards, Steven,Chan, Vicky,Nachtigall, Jason,Du, Hongwang,Noson, Kevin,Galan, Adam,Aay, Naing,Hanel, Art,Harrison, Amanda,Zhang, Jeff,Won, Kwang-Ai,Tam, Danny,Qian, Fawn,Wang, Tao,Finn, Patricia,Ogilvie, Kathleen,Rosen, Jon,Mohan, Raju,Larson, Christopher,Lamb, Peter,Nuss, John,Kearney, Patrick
scheme or table, p. 6773 - 6777 (2011/12/05)
A novel series of potent inhibitors of glucosylceramide synthase are described. The optimization of biochemical and cellular potency as well as ADME properties led to compound 23c. Broad tissue distribution was obtained following oral administration to mice. Thus 23c could be another useful tool compound for studying the effects of GCS inhibition in vitro and in vivo.
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
