title: Synthesis and bioactivity of 4-alkyl(aryl)thioquinazoline derivatives.
abstract: Some S'-substituted 4-alkyl(aryl)thioquinazoline derivatives were synthesized through thioetherification reaction of 4-chloroquinazolines 2 and thiol compounds 1 refluxed in acetone in the presence of K(2)CO(3). Their structures were verified by elemental analysis, IR, (1)H NMR, and (13)C NMR. The compounds were evaluated for their anti-proliferative activities against some cancer cells in vitro by MTT method. Among them, 3c, 3a, 3d, 3f, and 3l were highly effective against PC3 cells and 3a-3m showed weak activities against Bcap37 and BGC823 cells. The IC(50) value of 3c, 3a, 3d, 3f, and3l against PC3 cell was 1.8, 5.6, 8.1, 8.7, and 8.9 microM, respectively.
authors.affiliation: Center for Research and Development of Fine Chemicals, Key Laboratory of Green Pesticide and Bioengineering, Ministry of Education, Guizhou University, Guiyang 550025, PR China.
authors.forename: Song
authors.initials: S
authors.lastname: Yang
authors.forename: Zhi
authors.initials: Z
authors.lastname: Li
authors.forename: Linhong
authors.initials: L
authors.lastname: Jin
authors.forename: Baoan
authors.initials: B
authors.lastname: Song
authors.forename: Gang
authors.initials: G
authors.lastname: Liu
authors.forename: Jiang
authors.initials: J
authors.lastname: Chen
authors.forename: Zhuo
authors.initials: Z
authors.lastname: Chen
authors.forename: Deyu
authors.initials: D
authors.lastname: Hu
authors.forename: Wei
authors.initials: W
authors.lastname: Xue
authors.forename: Ruiqing
authors.initials: R
authors.lastname: Xu
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D048049:Extracellular Signal-Regulated MAP Kinases / Q000037:antagonists & inhibitors / Q000378:metabolism; D005260:Female; D006801:Humans; D020128:Inhibitory Concentration 50; D008297:Male; D015394:Molecular Structure; D010766:Phosphorylation / Q000187:drug effects; D000091402:Prohibitins; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013438:Sulfhydryl Compounds / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; C000717331:PHB2 protein, human; D000091402:Prohibitins; D011799:Quinazolines; D013438:Sulfhydryl Compounds; D048049:Extracellular Signal-Regulated MAP Kinases