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Alkoxy-functionalised dihydropyrimido[4,5- b ]quinolinones enabling anti-proliferative and anti-invasive agents.

Subham G PatelIra SharmaMehul P ParmarJoaquina NogalesChirag D PatelSavan S BhalodiyaDisha P ValaNiraj V ShahSourav BanerjeeHitendra M Patel
Published in: Chemical communications (Cambridge, England) (2024)
In this communication, we explored the synthesis of novel alkoxy-functionalised dihydropyrimido[4,5- b ]quinolinones using a microwave-assisted multicomponent reaction. All the synthesized molecules were screened for anti-proliferative and anti-invasive activity against glioblastoma cells. 5c shows the most potent anti-proliferative activity with a half maximal effective concentration of less than 3 μM against primary patient-derived glioblastoma cells. 5c effectively inhibited invasion and tumor growth of 3D primary glioma cultures in a basement membrane matrix. This suggests that the novel compounds could inhibit both the proliferation and invasive spread of glioma and they were selected for further study.
Keyphrases
  • induced apoptosis
  • cell cycle arrest
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  • endoplasmic reticulum stress
  • cell death
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  • anti inflammatory
  • resistance training