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Design, synthesis and biological evaluation of trinary benzocoumarin-thiazoles-azomethines derivatives as effective and selective inhibitors of alkaline phosphatase.
- Source :
-
Bioorganic chemistry [Bioorg Chem] 2019 Oct; Vol. 91, pp. 103137. Date of Electronic Publication: 2019 Jul 23. - Publication Year :
- 2019
-
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.<br /> (Copyright © 2019 Elsevier Inc. All rights reserved.)
- Subjects :
- Alkaline Phosphatase chemistry
Alkaline Phosphatase metabolism
Animals
COS Cells
Catalytic Domain
Cell Line, Tumor
Cell Proliferation drug effects
Chlorocebus aethiops
Coumarins chemical synthesis
Coumarins metabolism
Drug Design
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors metabolism
GPI-Linked Proteins antagonists & inhibitors
GPI-Linked Proteins chemistry
GPI-Linked Proteins metabolism
Humans
Hydrazones chemical synthesis
Hydrazones metabolism
Molecular Docking Simulation
Molecular Structure
Protein Binding
Structure-Activity Relationship
Thiazoles chemical synthesis
Thiazoles metabolism
Alkaline Phosphatase antagonists & inhibitors
Coumarins pharmacology
Enzyme Inhibitors pharmacology
Hydrazones pharmacology
Thiazoles pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1090-2120
- Volume :
- 91
- Database :
- MEDLINE
- Journal :
- Bioorganic chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 31400554
- Full Text :
- https://doi.org/10.1016/j.bioorg.2019.103137