On May 31, 2003, Kim, Dong Chan; Lee, Yeo Ran; Yang, Beom-Seok; Shin, Kye Jung; Kim, Dong Jin; Chung, Bong Young; Yoo, Kyung Ho published an article.Quality Control of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine The title of the article was Synthesis and biological evaluations of pyrazolo[3,4-d]pyrimidines as cyclin-dependent kinase 2 inhibitors. And the article contained the following:
A series of 1,4,6-trisubstituted pyrazolo[3,4-d]pyrimidines capable of selectively inhibiting CDK2 activity were synthesized by derivatization at C-4, C-6 and N-1 with various amines and lower alkyl groups. For above synthetic compounds, biol. evaluation was carried out and structure-activity relationship was examined In the series, 4-anilino compounds exhibited better CDK2 inhibitory activity and antitumor activity compared to 4-benzyl compounds Two compounds having a 3-fluoroaniline group at C-4 showed comparable or superior CDK2 inhibitory activity to those of olomoucine and roscovitine as reference compounds In general, the unsubstituted compounds at N-1 possessed higher potency than the substituted compounds for the CDK2 inhibitory activity. As for EGFR inhibitory activity, most compounds did not have a significant activity. Two compounds exhibited potent cell growth inhibitory activity against human cancer cell lines, but their CDK2 inhibitory activities were slightly poorer than olomoucine. The experimental process involved the reaction of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine(cas: 85426-79-5).Quality Control of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine
The Article related to pyrazolopyrimidine preparation cyclin dependent kinase 2 inhibitor, cdk2 inhibitor pyrazolopyrimidine preparation, egfr inhibitor pyrazolopyrimidine preparation, antitumor agent pyrazolopyrimidine preparation and other aspects.Quality Control of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics