Oh, CH Kim, HK Lee, SC Oh, C Yang, BS Rhee, HJ Cho, JH 2024-01-21T11:37:34Z 2024-01-21T11:37:34Z 2022-01-10 2001-11 0365-6233 https://pubs.kist.re.kr/handle/201004/140063 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 0.3 muM, 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. English WILEY-V C H VERLAG GMBH SELECTIVE INHIBITOR PURINE ANALOGS CDK INHIBITORS CDC2 KINASE ROSCOVITINE CANCER POTENT Synthesis and biological properties of C-2, C-8, N-9 substituted 6-(3-chloroanilino)purine derivatives as cyclin-dependent kinase inhibitors. Part II Article 10.1002/1521-4184(200112)334:11<345::AID-ARDP345>3.0.CO;2-1 1 ARCHIV DER PHARMAZIE, v.334, no.11, pp.345 - 350 ARCHIV DER PHARMAZIE 334 11 345 350 scie scopus 000173080100002 2-s2.0-0035668305 Chemistry, Medicinal Chemistry, Multidisciplinary Pharmacology & Pharmacy Pharmacology & Pharmacy Chemistry Article SELECTIVE INHIBITOR PURINE ANALOGS CDK INHIBITORS CDC2 KINASE ROSCOVITINE CANCER POTENT CDK2 inhibitor m-chloroanilinopurine cell cycle regulation antiproliferative effect