Shen Guang Huan, Kang Lien, Kim Eunae, Hong Joon Hee
BK-21 Project Team, College of Pharmacy, Chosun University, Kwangju, Republic of Korea.
Nucleosides Nucleotides Nucleic Acids. 2012;31(10):720-35. doi: 10.1080/15257770.2012.724134.
A very efficient synthetic route to novel 3'-hydroxymethyl 5'-deoxythreosyl phosphonic acid nucleosides was described. The discovery of threosyl phosphonate nucleoside (PMDTA, EC(50) = 2.53 μM) as a potent antihuman immunodeficiency virus (anti-HIV) agent has led to the synthesis and biological evaluation of 3'-modified 5'-deoxy versions of the threosyl phosphonate nucleosides. 3'-Hydroxymethyl 5 '-deoxythreosyl phosphonic acid nucleoside analogues 15, 19, 24, and 28 were synthesized from 1,3-dihydroxyacetone and tested for anti-HIV activity as well as cytotoxicity. The adenine analogue 19 exhibits moderate in vitro anti-HIV-1 activity (EC(50) = 10.2 μM).
描述了一种合成新型3'-羟甲基5'-脱氧苏糖基膦酸核苷的高效合成路线。苏糖基膦酸核苷（PMDTA，半数有效浓度（EC50）=2.53μM）作为一种有效的抗人类免疫缺陷病毒（抗HIV）药物被发现，这促使人们对3'-修饰的5'-脱氧苏糖基膦酸核苷进行合成和生物学评价。由1,3-二羟基丙酮合成了3'-羟甲基5'-脱氧苏糖基膦酸核苷类似物15、19、24和28，并对其抗HIV活性和细胞毒性进行了测试。腺嘌呤类似物19表现出中等程度的体外抗HIV-1活性（EC50=10.2μM）。
