17338-96-4Relevant articles and documents
Synthesis and biological properties of C-2, C-8, N-9 substituted 6-(3-chloroanilino)-purine derivatives as cyclin-dependent kinase inhibitors. Part II
Oh, Chang-Hyun,Kim, Hee-Kwon,Lee, Su-Chul,Oh, Changsok,Yang, Boem-Seok,Rhee, Hak June,Cho, Jung-Hyuck
, p. 345 - 350 (2007/10/03)
In this study, C-2, C-8, N-9 substituted 6-(3-chloroanilino)purine derivatives were synthesized and their inhibitory effects on cyclin-dependent kinases (CDK2, 4) as well as their cytotoxicities were evaluated. The effects of substituents at the C-2, C-8, and N-9 positions of the substituted purine were investigated. Among the compounds tested, [6-(3-chloroanilino)-2-(2-hydroxymethyl-4-hydroxypyrrolidyl)- 9-isopropylpurine] (4h) was the most active inhibitor of CDK2 with IC50 of 0.3μM i.e. a two-fold increased inhibitory activity as compared to roscovitine. Results from structure-activity relationship studies should allow the design of more potent and selective CDK2 inhibitors, which may provide an effective therapy for cancer or other CDK-dependent diseases.