Journal article icon

Journal article

Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles.

Abstract:

Substituted guanines and pyrimidines were tested as inhibitors of cyclin B1/CDK1 and cyclin A3/CDK2 and soaked into crystals of monomeric CDK2. O6-Cyclohexylmethylguanine (NU2058) was a competitive inhibitor of CDK1 and CDK2 with respect to ATP (Ki values: CDK1, 5 +/- 1 microM; CDK2, 12 +/- 3 microM) and formed a triplet of hydrogen bonds (i.e., NH-9 to Glu 81, N-3 to Leu 83, and 2-NH2 to Leu 83). The triplet of hydrogen bonding and CDK inhibition was reproduced by 2,6-diamino-4-cyclohexylmet...

Expand abstract
Publication status:
Published

Actions


Access Document


Publisher copy:
10.1021/jm990628o

Authors


Expand authors...
Journal:
Journal of medicinal chemistry
Volume:
43
Issue:
15
Pages:
2797-2804
Publication date:
2000-07-05
DOI:
EISSN:
1520-4804
ISSN:
0022-2623
URN:
uuid:82f0d53e-5dea-4583-8a6d-65df46847644
Source identifiers:
56920
Local pid:
pubs:56920

Terms of use


Metrics



If you are the owner of this record, you can report an update to it here: Report update to this record

TO TOP