A facile synthesis and biological activity of novel tetrahydrobenzo[4',5']thieno[3',2':5,6]pyrido[4,3-d]pyrimidin-4(3H)-ones.
The synthesis and biological activity of 2-substituted-8,9,10,11-tetrahydrobenzo[4',5']thieno[3',2':5,6] pyrido[4,3-d]pyrimidin-4(3H)-ones are described. Bioassay results indicated that these compounds have antifungal activity against Botrytis cinerea at a concentration of 50mg/L. In addition, compounds 5m and 5n were effective to both KB cells and their parent multidrug resistant KBv200 cells with the overexpression of ABCB1. For example, compound 5m showed the best inhibition against KB and KBv200 cells with IC(50) values of 17.4 and 25.4 microM, respectively.
Key Laboratory of Pesticide & Chemical Biology, Ministry of Education, College of Chemistry, Central China Normal University, Wuhan 430079, PR China.
Qingyun
Q
Ren
Yong-Ju
YJ
Liang
Hongwu
H
He
Liwu
L
Fu
Yucheng
Y
Gu
D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020171:Botrytis / Q000187:drug effects*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D018432:Drug Resistance, Multiple; D019008:Drug Resistance, Neoplasm; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007624:KB Cells; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D011744:Pyrimidinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D000935:Antifungal Agents; D000970:Antineoplastic Agents; D011744:Pyrimidinones; D013876:Thiophenes