Saneyoshi Hisao, Vu B Christie, Hughes Stephen H, Boyer Paul L, Sarafianos Stefan G, Marquez Victor E
Laboratory of Medicinal Chemistry, Center for Cancer Research, National Cancer Institute at Frederick, National Institutes of Health, Frederick, MD 21702, USA.
Nucleic Acids Symp Ser (Oxf). 2008(52):623-4. doi: 10.1093/nass/nrn315.
The conformationally locked carbocyclic nucleoside phosphonates 2 and 2' and key intermediates for the synthesis of 3 and 3' were prepared from a chiral cyclopentene derivative and epicholorohydrine, respectively. The structure of the nucleoside precursor 6 was confirmed by X-ray crystallography. These carbocyclic nucleoside phosphonates were designed to probe their binding interactions at the active site of HIV-1-RT.
构象锁定的碳环核苷膦酸酯2和2'以及用于合成3和3'的关键中间体分别由手性环戊烯衍生物和表氯醇制备。核苷前体6的结构通过X射线晶体学得以确证。设计这些碳环核苷膦酸酯以探究它们在HIV-1逆转录酶活性位点的结合相互作用。
