Ko Yun Jung, Choi Won Jun, Jun Jung Ha, Zhao Long Xuan, Jeong Lak Shin
Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul 120-750, Korea.
Nucleic Acids Symp Ser (Oxf). 2008(52):555-6. doi: 10.1093/nass/nrn281.
The structure of 2',3'-didehydro-2',3'-dideoxynucleosides (d4Ns) was applied to design the novel bioisosteric 4'-seleno-d4Ns as potential inhibitors of human immunodeficiency virus reverse transcriptase (HIV RT). Conversion of 2',3'-dihydroxyl groups of 4'-selenoribofuranosyl pyrimidines into the olefin was accomplished by treatment of cyclic 2',3'-thiocarbonate with 1,3-dimethyl-2-phenyl-1,3,2-diazaphospholidine.
将2'，3'-二脱氢-2'，3'-二脱氧核苷（d4Ns）的结构用于设计新型生物电子等排体4'-硒代-d4Ns，作为人类免疫缺陷病毒逆转录酶（HIV RT）的潜在抑制剂。通过用1,3-二甲基-2-苯基-1,3,2-二氮杂磷环戊烷处理环状2'，3'-硫代碳酸酯，将4'-硒代呋喃核糖基嘧啶的2'，3'-二羟基转化为烯烃。
