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Apr 2010 Bioorganic & medicinal chemistry letters

N-aryltriazole ribonucleosides with potent antiproliferative activity against drug-resistant pancreatic cancer.


Xia Y, Fan Y, Maggiani A, Rocchi P, Qu F, Iovanna JL, Peng L


Novel N-aryltriazole nucleosides were synthesized via Cu-mediated C-N cross-coupling reaction starting with 3-aminotriazole ribonucleoside and various boronic acids. Two of them exhibited potent apoptosis-related antiproliferative activity against the drug-resistant pancreatic cancer cell line MiaPaCa-2, with an increased potency compared to gemcitabine, the reference treatment for pancreatic cancer. A preliminary SAR study suggests that the appended N-aryl moiety and the substituent at its para-position, as well as the ribose sugar component, contribute considerably to the observed antiproliferative activity.

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