864655-05-0Relevant articles and documents
Design and Synthesis of Novel 2,4-Diamino-5-pyrazol-4-yl Pyrimidine Derivatives as Selective Tyro3 Kinase Inhibitors
Kim, Dukwoon,Lee, Kyung Won,Jung, Hyunseok,Kim, Miok,Lee, Joo-Youn,Lee, Yeonkyung,Hwang, Jong Yeon,Min, Youngki,Lee, Chang Hoon,Cho, Sung Yun
, p. 1101 - 1104 (2018)
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Discovery of 5-methylpyrimidopyridone analogues as selective antimycobacterial agents
Wu, Yu,Cheung, Chen-Yi,Zhou, Yang,Wang, Zhen,Tu, Zhengchao,Cook, Gregory M.,Lu, Xiaoyun
, (2021/10/08)
With the emergence of multidrug-resistant strains of Mycobacterium tuberculosis (MDR-TB) and extensive drug-resistant strains (XDR-TB), there is an urgent need to develop novel drugs for the treatment of tuberculosis. Here, we designed and synthesized a series of 5-methylpyrimidopyridone analogues as potential antitubercular agents. The most potent compound 6q exhibited a MIC value of 4 μM in vitro against Mycobacterium tuberculosis. The antitubercular activities of the synthesized compounds were impacted by the amantadine and 2-chlorophenyl groups, and were enhanced by the presence of 3-methyl(4-dimethylamino)piperidinylphenyl. Molecular modeling and binding studies suggest that PknB is the potential molecular target of 5-methylpyrimidopyridone compounds. This study provides insights for the future development of new antimycobacterial agents with novel mechanisms of action.
Novel Mps1 kinase inhibitors: From purine to pyrrolopyrimidine and quinazoline leads
Bursavich, Matthew G.,Dastrup, David,Shenderovich, Mark,Yager, Kraig M.,Cimbora, Daniel M.,Williams, Brandi,Kumar, D. Vijay
, p. 6829 - 6833 (2014/01/06)
Mps1, also known as TTK, is a mitotic checkpoint protein kinase that has become a promising new target of cancer research. In an effort to improve the lead-likeness of our recent Mps1 purine lead compounds, a scaffold hopping exercise has been undertaken.