Latest advances on regiospecific microwave-assisted synthesis of novel purine derivatives as antitumor agents

Abstract

Background: Breast cancer, a leading cause of mortality in women, warrants the development of biological evaluation of new anticancer agents. Objective: A novel series of (RS)-6-substituted-7 or 9-(2,3-dihydro-5H-1,4-benzodioxepin-3-yl)-7H- or -9H-purines and (RS) 2- and 6-substituted (RS)-9-(2,3-dihydro-1,4-benzoxathiin-3-ylmethyl)-9H-purine derivatives were synthesized and investigated in the human breast-cancer cell line MCF-7. Methods: The microwave-assisted organic synthesis has provided faster access to the target compounds with the advantage for the selective preparation of the N-7′ or N-9′ regioisomers. Results/conclusion: The anticarcinogenic potential of the target molecules is reported against the MCF-7 cancer cell line. The most active compounds were used to study the cell cycle distribution and apoptosis in the MCF-7 cell line. The results indicated that the anticancer activity for the most active compounds is correlated with their capability to induce apoptosis.

Keywords::

• antitumor compound
• microwave
• MCF-7
• 6-substituted purine
• apoptosis

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