Synthesis of Novel Series of Benzothieno [2,3-d] Pyrimidine Derivatives, Promising Anticancer Agents  

作　　者：Omer Khalid AI-Duaij Hend Nagah Hafez Abdel-Rhman Barakat Ahmed EI-Gazzar 

机构地区：[1]Department of Chemistry, Faculty of Science, Al-lmam Mohammad Ibn Saud Islamic University, Riyadh 11623, Kingdom of SaudiArabia [2]Photochemistry Department, National Research Centre, Cairo 12622, Egypt

出　　处：《Journal of Chemistry and Chemical Engineering》2013年第8期725-742,共18页化学与化工（英文版）

摘　　要：An extension of the authors＇ previous discovery of in vitro antitumor activity of substituted thino [2,3-d] prymidine derivatives is reported. The synthesis of some new spirothino [2,3-d] prymidine （4a-f）, imidazolidin, substituted prymidinyl and substituted thiazolidine thino [2,3-d] prymidine derivatives have been described. Thirteen of the obtained compounds were selected by the NCI and evaluated for their in vitro anticancer activity. Seven of the investigated compounds, 4a, 8a, 9a, （12a, b）, 14a and 15a, displayed high anticancer activity in the primary assay. These compounds have been selected for a full anticancer screening against a 60-cell panel assay where they showed non-selective broad spectrum and promising activity against all cancer cell lines. Compounds 12a and 12b proved to be the active members in this study compared to 5-fluorouracil and cyclophosphamide as reference drugs, respectively. Compounds 12a and 12b were identified as promising lead compounds, evaluated for their in-vitro antitumor activity.

关 键 词：Spiro thieno [2 3-d] prymidine THIAZOLIDINE thienoprymidine anticancer activity. 

分 类 号：S831.5[农业科学—畜牧学] S791.49[农业科学—畜牧兽医]