Microwave-Assisted Synthesis, Structure, and Preliminary Biological Evaluation of Novel 6-Methoxy-5,6-dihydro-5-azapurines. 2023

Alena I Siutkina, and Svetlana Kalinina, and Rongfang Liu, and Laura H Heitman, and Anna Junker, and Constantin G Daniliuc, and Dmitrii V Kalinin
Institute of Pharmaceutical and Medicinal Chemistry, University of Münster, 48149 Münster, Germany.

We herein disclose the microwave-assisted synthesis of previously unreported 6-methoxy-5,6-dihydro-5-azapurines, whose purine-like scaffold is promising for drug discovery. The method is simple, fast, and relies on easily accessible reagents such as trimethyl orthoformate, acetic acid, and aminotriazole-derived N,N'-disubstituted formamidines. The preliminary biological evaluation revealed that selected representatives of synthesized 6-methoxy-5,6-dihydro-5-azapurines dose-dependently reduce the viability of HepG2 and A549 cancer cells having little to no influence on five tested purinergic receptors.

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