synthesis and antiproliferative activities of 5-azacytidine analogues in human leukemia cells5-azacytidine类似物的合成和抗增殖活动在人类白血病细胞.pdf

Molecules 2008, 13, 1487-1500; DOI: 10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /molecules Article Synthesis and Antiproliferative Activities of 5-Azacytidine Analogues in Human Leukemia Cells 1 1 1 1 1 2 Gang Guo , Gang Li , Dan Liu , Qian-jiao Yang , Yu Liu , Yong-kui Jing and Lin-xiang 1 Zhao * 1 Shenyang Pharmaceutical University, Shenyang, 110016, P. R. China; E-mails: guogan(Guo); ligang2001_21@ (Li); sammyld@163.com(Liu); yangqianjiao102@ (Yang); liforever7944@ (Liu) 2 Mount Sinai School of Medicine, One Gustave L. Levy Place, New York, NY 10029, USA; E-mail: yongkui.jing@ * Author to whom correspondence should be addressed. E-mail: zhaolinxiang@; Tel.: (+86)24 Fax: (+86)24 Received: 20 June 2008; in revised form: 15 July 2008 / Accepted: 15 July 2008 / Published: 23 July 2008 Abstract: Twenty-six 5-azacytidine analogues have been synthesized, including 4-amino- 6-alkyl-1-pyranosyl/ribofuranosyl-1,3,5-triazin-2(1H)-ones 1a-j, 6-amino-4-alkyl/aryl-1- pyranosyl/ribofuranosyl-1,3,5-triazin-2(1H)-ones 2a-f and 4-amino-6-alkyl-1,3,5-triazin-2- yl-1-thio-pyranosides/ribofuranosides 3a-j. The antiproliferative activities of these synthetic analogues were investigated in human leukemia HL-60 cells. Ribofuranosyl S- nucleoside 3a, a bioisostere of 5-azacytidine, had a similar antiproliferative ability as that of the latter.