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Synthesis and Biological Activities of Novel s-Triazine Bridged Dinucleoside Analogs.pdf
FULLPAPER
SynthesisandBiologicalActivitiesofNovels-TriazineBridged
DinucleosideAnalogs
Shen，Fengjuan (申凤娟) Li，Xiaoliu (李小六) Zhang，Xiaoyuan(张晓嫒)
Qin，Zhanbin(秦占斌) Yin，Qingmei。(殷庆梅) Chen，Hua(陈华)
Zhang，Jinchao。(张金超)
“KeyLaboratoryofChemicalBiologyofHebeiProvince，CollegeofChemistryandEnvironmentalScience，Hebei
University，Baoding，Hebei071002，China
CollegeofScience，HebeiUniversityofScience＆Technology，Shijiazhuang，Hebei050018，China
A seriesofnoveldinucleosideslinkedby —triazineweresynthesizedviathenucleophilicsubstitutionreaction
ofaminonucleosideandcyanuricchlorideinTHF／H20．Thebiologicalactivitiesofthesenoveldinucleosideana—
logsagainstHIV—RT，HeLaandA一549celllinesinvitrowereevaluated．
Keywords dinucleoside，—triazine，HIV—RT inhibition，cyanuricchloride
Introduction cleosideanalogscontainingan —triazinemoiety，suchas
Decitabine(aza—dCyd)(A)andVidaza(aza—Cyd)(B)
Thesynthesisofnucleosideanalogshasbeenthehot
(Figure1)，havebeenapprovedbyFDAtobeusedin
topicinthepastdecadesduetotheirpotentialapplica．
clinicasanticanceragents．
tionasanticancerand antiviraltherapeuticagents．To
meettheever—growingrequirementsinthediscoveryof
new drugs，variOHSmodificationson theheterocyclic
basesand／orthesugarmoietyhavebeen approached， N
suchasheterocyclic—sugarnucleosides，。spirocyclicnu—
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