Synthesis and antitumor activities of pyrimidines.
- Author:
Wen-wei YOU
1
;
Pei-liang ZHAO
;
Min ZOU
;
Zhong-zhen ZHOU
;
An-na DUAN
;
Shu-guang WU
Author Information
- Publication Type:Journal Article
- MeSH: Antineoplastic Agents; chemical synthesis; chemistry; pharmacology; Cell Line, Tumor; Drug Screening Assays, Antitumor; Humans; Pyrimidines; chemical synthesis; chemistry; pharmacology; Structure-Activity Relationship
- From: Journal of Southern Medical University 2011;31(5):875-877
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVETo synthesize cyclin-dependent kinase (CDKs) inhibitors and assay their antitumor activities.
METHODSA series of pyrimidines containing different arylamino and 1-(methylsulfonyl)piperidin moieties were designed by combining the segments 1-(methylsulfonyl)piperidin and pyrimidine heterocycles according to the super-position principle of the reinforcement of biological activities.
RESULTSTheir structures were characterized by MS and 1H NMR spectra and all the synthesized compounds were screened for their antimicrobial activity with MTT assay.
CONCLUSIONThe preliminary bioassay showed that compound 3 b displayed good antitumor activity (IC(50)=13.6 µmol/L). The preliminary structure activity relationship analysis of these analogues suggest that the steric factor may have important impact on the anti-tumor activity.
