title: Synthesis and antitumor activity of novel ribonucleosides with C-5 OH replaced by a diaminopyrimidinyl group.
abstract: A series of novel ribonucleosides with C-5 OH replaced by a diaminopyrimidinyl group were synthesized by successively nucleophilic substitutions of 5'-deoxy-5'-amino-ribonucleosides with 2,4-dichloropyrimidine and then with various fatty amines under microwave irradiation. Their anticancer activities in vitro were preliminarily evaluated. Compounds 7a and 8a only exhibited anticancer activity against A549 cell line with the IC(50) values of 10.73 and 10.99 μM, respectively. In addition, 7h and 8h showed potent activities against both A549 and Hela cell lines with the IC(50) values of 12.71, 8.55 and 8.44, 5.55 μM, respectively.
authors.affiliation: Key Laboratory of Chemical Biology of Hebei Province, College of Chemistry and Environmental Science, Hebei University, Baoding, China.
authors.forename: Kerang
authors.initials: K
authors.lastname: Wang
authors.forename: Ling
authors.initials: L
authors.lastname: Wu
authors.forename: Zhanbin
authors.initials: Z
authors.lastname: Qin
authors.forename: Xinhao
authors.initials: X
authors.lastname: Yan
authors.forename: Xiaoliu
authors.initials: X
authors.lastname: Li
authors.forename: Hua
authors.initials: H
authors.lastname: Chen
authors.forename: Pingzhu
authors.initials: P
authors.lastname: Zhang
authors.forename: Jinchao
authors.initials: J
authors.lastname: Zhang
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008872:Microwaves; D011743:Pyrimidines / Q000737:chemistry*; D012263:Ribonucleosides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D011743:Pyrimidines; D012263:Ribonucleosides; C513879:2,4-dichloropyrimidine