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Microwave-assisted multicomponent synthesis of antiproliferative 2,4-dimethoxy-tetrahydropyrimido[4,5- b ]quinolin-6(7 H )-ones.

Subham G PatelAday González-BakkerRuturajsinh M ValaParas J PatelAdrián PuertaApoorva MalikRakesh K SharmaJosé Manuel PadrónHitendra M Patel
Published in: RSC advances (2022)
In this study, we demonstrate a simple, highly efficient, rapid and convenient series of 2,4-dimethoxy-tetrahydropyrimido[4,5- b ]quinolin-6(7 H )-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 in silico ADMET profile. Furthermore, 4h, 4o, 4q and 4v also show drug-likeness properties by obeying drug-like filters.
Keyphrases
  • highly efficient
  • molecular docking
  • endothelial cells
  • mass spectrometry
  • randomized controlled trial
  • adverse drug
  • high speed
  • induced pluripotent stem cells
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