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The reaction of the azidothymidine (AZT) with the 30-propynoylated derivative of 3,28-<i>O</i>,<i>O</i>′-diacetylbetulin gave a 1,4-disubstituted 1,2,3-triazole. The chemical structure of new derivative was characterized by ¹H NMR, ¹³C NMR and HR-MS. The triterpene-AZT conjugate was tested against a human cancer cell lines such as glioblastoma (SNB-19), amelanotic melanoma (C-32), ovarian adenocarcinoma (SKOV-3) and breast cancer (T47D, and MCF-7). 3′-[4-({[3β,28-Bis(acetyloxy)lup-20(29)-en-30-yl]oxy}carbonyl)-1<i>H</i>-1,2,3-triazol-1-yl]-3′-deoxythymidine shown significant activity against MCF-7 cells, with an IC₅₀ value of 4.37 µM.