期刊
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
卷 23, 期 17, 页码 -出版社
MDPI
DOI: 10.3390/ijms23179704
关键词
asymmetric synthesis; carbocyclic nucleosides; HSV-1 thymidine kinase; enzymatic assays
资金
- Spanish Ministry of Economy, Industry, and Competitiveness (MINECO) [CTQ2016-75363-R, PID2019-106403RB-I00]
- European Fund for Regional Development (FEDER)
The enantioselective preparation of the two isomers of 4-hydroxy-2-cyclohexanone derivatives was achieved through asymmetric transfer hydrogenation reactions. A stereoselective route to a cytosine analogue was described, showing selectivity for herpes simplex virus TKs.
The enantioselective preparation of the two isomers of 4-hydroxy-2-cyclohexanone derivatives 1a,b was achieved, starting from a common cyclohexenone, through asymmetric transfer hydrogenation (ATH) reactions using bifunctional ruthenium catalysts. From these versatile intermediates, a stereoselective route to a cytosine analogue built on a bicyclo [4.1.0]heptane scaffold is described. Nucleoside kinase activity assays with this cyclopropyl-fused cyclohexane nucleoside, together with other related nucleosides (2a-e), were performed, showing that thymine- and guanine-containing compounds have affinity for herpes simplex virus Type 1 (HSV-1) thymidine kinase (TK) but not for human cytosolic TK-1, thus pointing to their selectivity for herpetic TKs but not cellular TKs.
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