Syntheses and Antiproliferative Evaluation of 6-Thienyl, 6-Polyphenyl Aryl and 6-Naphthyl Derivatives of 2,4-Diaminopyrido [3,2-d] pyramidine as Non-classical Antifolate Targeting DHFR

• Published in: Chemical research in Chinese universities Vol. 33; no. 4; pp. 559 - 568
• Main Authors: Yang, Jiajia, Wang, Meng, Li, Xia, Fan, Ningning, Xue, Liangmin, Li, Hao, Tian, Chao, Wang, Xiaowei, Liu, Junyi, Zhang, Zhili
• Format: Journal Article
• Language: English
• Published: Changchun Jilin University and The Editorial Department of Chemical Research in Chinese Universities 01.08.2017; Springer Nature B.V
• Subjects: Analytical Chemistry; Antibacterial materials; Anticancer properties; Antiproliferatives; Aromatic compounds; Chemistry; Chemistry and Materials Science; Chemistry/Food Science; Derivatives; Dihydrofolate reductase; Docking; In vitro methods and tests; Inorganic Chemistry; Organic Chemistry; Physical Chemistry; 二氢叶酸还原酶; 体外抗肿瘤活性; 嘧啶; 增殖; 衍生物; 设计合成; 评价; 非经典; Antimicrobial; Dihydrofolate reductase(DHFR); Non-classical antifolate; Antitumor

A series of 6-thienylethenyl, 6-polyphenyl arylethenyl, 6-thienylethyl and 6-polyphenyl arylethyl deriva- tives of 2,4-diaminopyrido[3,2-d]pyrimidine for targeting dihydrofolate reductase（DHFR） was designed and synthe- sized as non-classical antifolates in order to overcome drug resistance. The comp...