17465-94-0Relevant articles and documents
Synthesis and herbicidal evaluation of aryloxyphenoxypropiona te derivatives containing purine moiety
Shi, Jianjun,Ren, Guihua,Dai, Zhimeng,Wu, Ningjie,Weng, Jianquan,Xu, Tianming,Liu, Xinghai,Tan, Chengxia
, p. 15 - 20 (2018)
series of purinoxyphenoxypropionates were designed and synthesized by introducing 8-(trifluoromethyl)-9H-purine into the aryloxyphenoxypropionate backbone. Methods: The products were characterized by 1H NMR and HRMS. Results and Conclusion: Preliminary bioassays indicated that most of the compounds exhibited good herbicidal activity at 200 mg/L.
An efficient synthesis of 4,6-substituted pyrrolo[3,2-d]pyrimidines by silver-catalyzed cyclization of acetylene amine
Xie, Rui,Hu, Ying,Wan, Huixin,Hu, Yanwei,Chen, Shaohua,Zhang, Shilei,Zhang, Yinan
supporting information, p. 2418 - 2421 (2016/05/19)
A silver catalyzed cyclization of acetylene amine was developed to synthesize 4,6-substituted pyrrolo[3,2-d]pyrimidine, a bioactive isosteric scaffold of purine. Starting from simple commercially available acetylenes and pyrimidines, the method was found
Enhanced selectivity for inhibition of analog-sensitive protein kinases through scaffold optimization
Zhang, Chao,Shokat, Kevan M.
, p. 5832 - 5838 (2008/02/03)
The ability to inhibit any protein kinase of interest with a small molecule is enabled by a combination of genetics and chemistry. Genetics is used to modify the active site of a single kinase to render it distinct from all naturally occurring kinases. Next, organic synthesis is used to develop a small molecule, which does not bind to wild-type kinases but is a potent inhibitor of the engineered kinase. This approach, termed chemical genetics, has been used to generate highly potent mutant kinase-specific inhibitors based on a pyrazolopyrimidine scaffold. Here, we asked if the selectivity of the resulting pyrazolopyrimidines could be improved, as they inhibit several wild-type kinases with low-micromolar IC50 values. Our approach to improve the selectivity of allele-specific inhibitors was to explore a second kinase inhibitor scaffold. A series of 6,9-disubstituted purines was designed, synthesized, and evaluated for inhibitory activity against several kinases in vitro and in vivo. Several purines proved to be potent inhibitors against the analog-sensitive kinases and exhibited greater selectivity than the existing pyrazolopyrimidines.
