Synthesis and anticancer activity of N-9- and N-7- substituted 1,2,3 triazole analogues of 2,6-di-substituted purine


A library of N-9- and N-7-substituted 1,2,3 triazole analogues were generated on the 2,6-di-substituted purine upon reaction with various substituted aromatic azides. The synthesised analogues were screened for in vitro cytotoxic activity against various human cancer cell lines like (HCT-1 (colon), THP-1 (leukaemia), IMR-32 (neuroblastoma) and A-549 (lung)). From the bioassay results, it was observed that even though most of the synthesized derivatives exhibited a good potency against various screened cancer cell lines, but few of the analogues like 9a, 9b and 9e were found to be the most potent analogues in the series, with compound 9a showing IC50 values of 0.08 and 0.4 μM against THP-1 and A-549 cell lines, respectively.

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Fig. 1
Scheme 1
Fig. 2
Fig. 3



Phenyl ring


Benzyl amine


Triazole ring


Purine ring


Ethanol amine






Methylene group attached to benzene ring of benzyl amine


Methylene group attached to Triazole ring


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We thank University of Pretoria for providing postdoctoral fellowship to JK.

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Correspondence to Jabeena Khazir.

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Khazir, J., Mir, B.A., Chashoo, G. et al. Synthesis and anticancer activity of N-9- and N-7- substituted 1,2,3 triazole analogues of 2,6-di-substituted purine. Med Chem Res 29, 33–45 (2020).

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  • 2,6 Dichloropurine
  • Cycloaddition
  • 1,2,3 triazoles
  • anticancer