930089-58-0Relevant academic research and scientific papers
Novel and orally active 5-(1,3,4-oxadiazol-2-yl)pyrimidine derivatives as selective FLT3 inhibitors
Ishida, Hiroshi,Isami, Shoichi,Matsumura, Tsutomu,Umehara, Hiroshi,Yamashita, Yoshinori,Kajita, Jiro,Fuse, Eiichi,Kiyoi, Hitoshi,Naoe, Tomoki,Akinaga, Shiro,Shiotsu, Yukimasa,Arai, Hitoshi
, p. 5472 - 5477 (2008)
5-(1,3,4-Oxadiazol-2-yl)pyrimidine derivative 1 was identified as a new class of FLT3 inhibitor from our compound library. With the aim of enhancement of antitumor activity of 2 prepared by minor modification of1, structure optimization of side chains at the 2-, 4-, and 5-positions of the pyrimidine ring of 2 was performed to improve the metabolic stability. Introduction of polar substituents on the 1,3,4-oxadiazolyl group contributed to a significant increase in the metabolic stability. As a result, a series of compounds showed increased efficacy against MOLM-13 xenograft model in mice by oral administration.
