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Bioorg Chem. 2019 Oct;91:103137. doi: 10.1016/j.bioorg.2019.103137. Epub 2019 Jul 23.

Design, synthesis and biological evaluation of trinary benzocoumarin-thiazoles-azomethines derivatives as effective and selective inhibitors of alkaline phosphatase.

Author information

1
Department of Chemistry, Quaid-i-Azam University, 45320 Islamabad, Pakistan.
2
Centre for Advanced Drug Research, COMSATS University Islamabad, Abbottabad Campus, Abbottabad 22060, Pakistan.
3
Department of Chemistry, Quaid-i-Azam University, 45320 Islamabad, Pakistan. Electronic address: asaeed@qau.edu.pk.
4
Department of Chemistry, Allama Iqbal Open University, Islamabad, Pakistan.
5
Département de microbiologie-infectiologie et d'immunologie, Faculté de Médecine, Université Laval, Québec, QC G1V 0A6, Canada; Centre de Recherche du CHU de Québec - Université Laval, Québec, QC G1V 4G2, Canada.
6
Centre for Advanced Drug Research, COMSATS University Islamabad, Abbottabad Campus, Abbottabad 22060, Pakistan. Electronic address: drjamshed@cuiatd.edu.pk.

Abstract

Design, synthesis and characterization of new trinary Benzocoumarin-Thiazoles-Azomethine derivatives having three bioactive scaffolds in a single structural unit were carried out. The newly synthesized molecules were investigated for the inhibitory activity on human tissue nonspecific alkaline phosphatase (h-TNAP) and human intestinal alkaline phosphatase (h-IAP) isozymes. All the tested compounds exhibited the potent inhibition profile on both isozymes of alkaline phosphatase i.e., h-TNAP and h-IAP. Molecular docking studies were performed to explore the putative binding mode of interactions of selective inhibitors. Moreover, the synthesized derivatives were evaluated against cervical cancer cell line, HeLa and a few compounds exhibited significant inhibition in the range of 21.0-69.7%. The derivatives can be potential and selective alkaline phosphatase inhibitors for future studies.

KEYWORDS:

Anticancer; Azomethine; Coumarin; Design; Human intestinal alkaline phosphatase; Synthesis; Thiazole; Tissue-nonspecific alkaline phosphatase

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