2. Academic Validation
  3. Biologically active perspective synthesis of heteroannulated 8-nitroquinolines with green chemistry approach

Biologically active perspective synthesis of heteroannulated 8-nitroquinolines with green chemistry approach

  • Bioorg Med Chem Lett. 2017 Apr 1;27(7):1538-1546. doi: 10.1016/j.bmcl.2017.02.042.
Thangaraj Arasakumar 1,  Sadasivam Mathusalini 2,  Subashini Gopalan 2,  Selvaraj Shyamsivappan 2,  Athar Ata 3,  Palathurai Subramaniam Mohan 4
Affiliations

Affiliations

  • 1 School of Chemical Sciences, Bharathiar University, Coimbatore 641 046, Tamil Nadu, India; Department of Chemistry, Richardson College for the Environmental Science Complex, The University of Winnipeg, 599 Portage Avenue, Winnipeg, Manitoba R3B 2G3, Canada.
  • 2 School of Chemical Sciences, Bharathiar University, Coimbatore 641 046, Tamil Nadu, India.
  • 3 Department of Chemistry, Richardson College for the Environmental Science Complex, The University of Winnipeg, 599 Portage Avenue, Winnipeg, Manitoba R3B 2G3, Canada. Electronic address: a.ata@uwinnipeg.ca.
  • 4 School of Chemical Sciences, Bharathiar University, Coimbatore 641 046, Tamil Nadu, India. Electronic address: psmohan59@gmail.com.
PMID: 28262524 DOI: 10.1016/j.bmcl.2017.02.042
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.

Keywords

Antibacterial; Anticancer; Antioxidant; Molecular docking; Pyrano[3,2-c]quinoline; Pyrazolo[4,3-c]quinoline.

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