Synthesis and biological evaluation of novel 2,4,5-substituted pyrimidine derivatives for anticancer activity.
A series of novel 2,4,5-substituted pyrimidine derivatives were synthesized and evaluated for inhibition against the human hepatocellular carcinoma BEL-7402 cancer cell line. Several compounds showed potent inhibition with an IC(50) value less than 0.10 microM. Structure-activity relationships for this class of compounds at the 2- and 5-position of the pyrimidine scaffold have been elucidated. The most active compound 7gc showed good inhibition of several different human cancer cell lines with IC(50) values from 0.024 to 0.55 microM.
Xie
Fuchun
F
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Medicinal Chemistry, Shanghai, China.
Zhao
Hongbing
H
Zhao
Lizhi
L
Lou
Liguang
L
Hu
Youhong
Y
D000970:Antineoplastic Agents / Q000138:chemical synthesis; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020128:Inhibitory Concentration 50; D008113:Liver Neoplasms / Q000188:drug therapy / Q000473:pathology; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D011743:Pyrimidines