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      https://www.ias.ac.in/article/fulltext/jcsc/126/04/1091-1105

    • Keywords

       

      Amide; phenol/catechol; Growth kinetics; T98G cell; In-silico Pharmacokinetics.

    • Abstract

       

      Several pyridine-amide compounds appended with phenol/catechol groups are synthesized. These compounds consist of protected or deprotected phenol/catechol groups and offer pyridine, amide, and phenol/catechol functional groups. All compounds have been well-characterized by various spectroscopic methods, elemental analysis, thermal studies, and crystallography. The biological activities of all compounds were investigated while a few compounds significantly decreased the metabolic viability, growth and clonogenicity of T98G cells in dose dependent manner. Accumulation of ROS was observed in T98G cells, which displayed a compromised redox status as evident from increased cellular Caspase 3/7 activity and formation of micronuclei. The in silico pharmacokinetic studies suggest that all compounds have good bioavailability, water solubility and other drug-like parameters. A few compounds were identified as the lead molecules for future investigation due to their: (a) high activity against T98G brain, H-460 lung, and SNU-80 thyroid cancer cells; (b) low cytotoxicity in non-malignant HEK and MRC-5 cells; (c) low toxic risks based on in silico evaluation; (d) good theoretical oral bioavailability according to Lipinski ‘rule of five’ pharmacokinetic parameters; and (e) better drug-likeness and drug-score values.

    • Author Affiliations

       

      Afsar Ali1 Deepak Bansal1 Nagendra K Kaushik2 Neha Kaushik2 Neha Kaushik1 Eun Ha Choi2 Rajeev Gupta1

      1. Department of Chemistry, University of Delhi, Delhi 110 007, India
      2. Plasma Bioscience Research Center, Kwangwoon University, Seoul 139 701, South Korea
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    • Supplementary Material

       
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