Patel Subham G, González-Bakker Aday, Vala Ruturajsinh M, Patel Paras J, Puerta Adrián, Malik Apoorva, Sharma Rakesh K, Padrón José M, Patel Hitendra M
Department of Chemistry, Sardar Patel University Vallabh Vidyanagar 388120 Gujarat India
BioLab, Instituto Universitario de Bio-Orgánica Antonio González (IUBO-AG), Universidad de La Laguna La Laguna E-38206 Spain.
RSC Adv. 2022 Oct 25;12(47):30404-30415. doi: 10.1039/d2ra04669e. eCollection 2022 Oct 24.
In this study, we demonstrate a simple, highly efficient, rapid and convenient series of 2,4-dimethoxy-tetrahydropyrimido[4,5-]quinolin-6(7)-ones 4a-v. Microwave irradiation facilitates the one-pot multicomponent reaction of different aromatic aldehydes, 6-amino-2,4-dimethoxypyrimidine and dimedone using glacial acetic acid. Metal-free multicomponent synthesis, shorter reaction time, higher product yield, easy product purification without column chromatography and outstanding green credential parameters are the key features of this protocol. We analysed 4a-v against six human tumour cell lines for antiproliferative activity. 4h, 4o, 4q and 4v show good antiproliferative activity with a good ADMET profile. Furthermore, 4h, 4o, 4q and 4v also show drug-likeness properties by obeying drug-like filters.
在本研究中，我们展示了一系列简单、高效、快速且便捷的2,4-二甲氧基-四氢嘧啶并[4,5-]喹啉-6(7)-酮4a-v。微波辐射促进了不同芳香醛、6-氨基-2,4-二甲氧基嘧啶和双甲酮在冰醋酸存在下的一锅多组分反应。无金属多组分合成、较短的反应时间、较高的产物收率、无需柱色谱即可轻松纯化产物以及出色的绿色认证参数是该方案的关键特征。我们分析了4a-v对六种人类肿瘤细胞系的抗增殖活性。4h、4o、4q和4v表现出良好的抗增殖活性以及良好的ADMET特性。此外，4h、4o、4q和4v通过符合类药筛选标准还表现出类药性质。
