Nucleoside analogues show a variety of biological activities. To prepare new purine nucleoside analogues that could inhibit the proliferation of tumor cells and resist enzyrne hydrolysis, we designed and synthesized 1...Nucleoside analogues show a variety of biological activities. To prepare new purine nucleoside analogues that could inhibit the proliferation of tumor cells and resist enzyrne hydrolysis, we designed and synthesized 15 different L-5'noraristeromycin analogues, in which thioether, sulfoxide or sulfone function was introduced to replace the 5'-hydroxymethyl group. Their anti-tumor activities were assayed in vitro. One compound showed potent anti-tumor activity.展开更多
Dideoxy-2'-fluoro-3'-hydroxymethylarabinofuranosylthymine 10 and cytosine 12 were synthesized from L-xylose and were found to be inactive against HIV-1 in acutely infected lymphocytes.
The synthesis of novel nucleoside analog (3R)-2,3-dideoxy-3-(N-hydroxy-N- methylamino)-L-arabinofuranosyl uracil was studied. A twelve-step synthetic route, started from L-ascorbic acid, was designed, and the final pr...The synthesis of novel nucleoside analog (3R)-2,3-dideoxy-3-(N-hydroxy-N- methylamino)-L-arabinofuranosyl uracil was studied. A twelve-step synthetic route, started from L-ascorbic acid, was designed, and the final product was obtained in 20.8% yield.展开更多
基金National Natural Science Foundation of China(Grant No.20672010)
文摘Nucleoside analogues show a variety of biological activities. To prepare new purine nucleoside analogues that could inhibit the proliferation of tumor cells and resist enzyrne hydrolysis, we designed and synthesized 15 different L-5'noraristeromycin analogues, in which thioether, sulfoxide or sulfone function was introduced to replace the 5'-hydroxymethyl group. Their anti-tumor activities were assayed in vitro. One compound showed potent anti-tumor activity.
文摘Dideoxy-2'-fluoro-3'-hydroxymethylarabinofuranosylthymine 10 and cytosine 12 were synthesized from L-xylose and were found to be inactive against HIV-1 in acutely infected lymphocytes.
文摘The synthesis of novel nucleoside analog (3R)-2,3-dideoxy-3-(N-hydroxy-N- methylamino)-L-arabinofuranosyl uracil was studied. A twelve-step synthetic route, started from L-ascorbic acid, was designed, and the final product was obtained in 20.8% yield.