新型6-甲氧基-5,6-二氢-5-氮杂嘌呤的微波辅助合成、结构及初步生物学评价
Microwave-Assisted Synthesis, Structure, and Preliminary Biological Evaluation of Novel 6-Methoxy-5,6-dihydro-5-azapurines.
作者信息
Siutkina Alena I, Kalinina Svetlana, Liu Rongfang, Heitman Laura H, Junker Anna, Daniliuc Constantin G, Kalinin Dmitrii V
机构信息
Institute of Pharmaceutical and Medicinal Chemistry, University of Münster, 48149 Münster, Germany.
Institute of Food Chemistry, University of Münster, 48149 Münster, Germany.
出版信息
ACS Omega. 2023 Apr 5;8(15):14097-14112. doi: 10.1021/acsomega.3c00765. eCollection 2023 Apr 18.
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 ,'-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.
我们在此公开了微波辅助合成此前未报道的6-甲氧基-5,6-二氢-5-氮杂嘌呤，其嘌呤样骨架在药物发现方面颇具前景。该方法简单、快速，且依赖于诸如原甲酸三甲酯、乙酸和氨基三唑衍生的α,α'-二取代甲脒等易于获得的试剂。初步生物学评估表明，合成的6-甲氧基-5,6-二氢-5-氮杂嘌呤的选定代表物剂量依赖性地降低了HepG2和A549癌细胞的活力，而对五种测试的嘌呤能受体几乎没有影响。
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