AI Article Synopsis

  • A new series of pyrazolo[4,3-c]quinoline and pyrano[3,2-c]quinoline derivatives were created using microwave synthesis, achieving moderate to good yields.
  • The compounds were tested for antibacterial properties, with notable effectiveness against both Gram-positive and Gram-negative bacteria, while also showing varying levels of antioxidant activity, particularly compound 9d.
  • Cytotoxicity evaluations indicated that most compounds had moderate to good effectiveness against breast and lung cancer cell lines, with compound 9i showing significant cytotoxic effects and promoting cell death through apoptosis.

Article Abstract

A new class of pyrazolo[4,3-c]quinoline (5a-i, 7a-b) and pyrano[3,2-c]quinoline (9a-i) derivatives were designed and synthesized in moderate to good yields by microwave conditions. To enhance the yield of pyrano[3,2-c]quinoline derivatives, multicomponent one-pot synthesis has been developed. The synthesized compounds were identified by spectral and elemental analyses. Compounds 9a and 9i showed good antibacterial activity against Gram-positive and Gram-negative bacterial strains. All of the new compounds exhibited weak to moderate antioxidant activity, compound 9d exerted significant antioxidant power. The cytotoxicity of these compounds were also evaluated against MCF-7 (breast) and A549 (Lung) cancer cell lines. Most of the compounds displayed moderate to good cytotoxic activity against these cell lines. Compound 9i was found to be significantly active in this assay and also induced cell death by apoptosis. Molecular docking studies were carried out using EGFR inhibitor in order to determine the molecular interactions.

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http://dx.doi.org/10.1016/j.bmcl.2017.02.042DOI Listing

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