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Thiosemicarbazone Complexes as Versatile Medicinal Chemistry Agents: A Review
Subject area: Science,Engineering and Technology · Area of research: Chemistry
Abstract
Thiosemicarbazone complexes, known for their significant versatility in medicinal chemistry, are a class of coordination compounds derived from thiosemicarbazone ligands that possess a remarkable ability to chelate with transition metals, and their extensive exploration has revealed their theoretical and conceptual potential to exhibit wide-ranging pharmacological properties such as anticancer, antimicrobial, antioxidant, antiviral, and antifungal activities, attributed to their ability to interfere with crucial biological pathways such as ribonucleotide reductase inhibition, topoisomerase II suppression, oxidative stress induction through reactive oxygen species generation, and interference with mitochondrial functions, which is further enhanced by the incorporation of various transition metals like copper, zinc, palladium, platinum, and iron, as these metals stabilize the ligand structure and augment their bioavailability, selectivity, and efficacy while minimizing off-target effects, with research restricted to September 2020 emphasizing that the structural diversity of thiosemicarbazones, achieved through ligand modifications such as the incorporation of heterocyclic moieties or hydrophobic groups, critically influences their biological activity by modulating metal coordination geometry, electronic properties, and lipophilicity, thereby optimizing their pharmacokinetics and pharmacodynamics, and their wide applicability in theoretical models, including docking studies and QSAR analyses, has provided valuable insights into their mechanism of action at the molecular level, with conceptual advancements focusing on their dual role as cytotoxic agents and enzyme inhibitors, making them promising candidates for the development of targeted therapeutic agents, while their ability to form stable complexes under physiological conditions has led to their evaluation as imaging agents and sensors in diagnostic applications, and the reviewed studies, sourced from comprehensive theoretical investigations and reviews indexed in established databases such as PubMed, Scopus, Web of Science, and Embase, collectively underscore the necessity for further refinement of synthetic strategies and ligand design to enhance their specificity and reduce potential toxicity, with the theoretical framework provided by quantum chemical calculations and molecular modeling offering a deeper understanding of their structure-activity relationships, highlighting the need for innovative approaches to translate these findings into clinical applications that leverage their unique coordination chemistry to address challenges in drug resistance and bioavailability in the future development of advanced thiosemicarbazone-based therapeutics.
Keywords
Thiosemicarbazone complexes, Medicinal chemistry, Transition metal coordination, Pharmacological properties, Structure-activity relationships (SAR), Therapeutic agent development
References
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How to cite this paper
@article{1702305,
author = {Dr. N. Y. Badannavar},
title = {Thiosemicarbazone Complexes as Versatile Medicinal Chemistry Agents: A Review},
journal = {Iconic Research And Engineering Journals},
year = {2020},
volume = {3},
number = {11},
pages = {341-351},
issn = {2456-8880},
url = {https://www.irejournals.com/formatedpaper/1702305.pdf},
abstract = {Thiosemicarbazone complexes, known for their significant versatility in medicinal chemistry, are a class of coordination compounds derived from thiosemicarbazone ligands that possess a remarkable ability to chelate with transition metals, and their extensive exploration has revealed their theoretical and conceptual potential to exhibit wide-ranging pharmacological properties such as anticancer, antimicrobial, antioxidant, antiviral, and antifungal activities, attributed to their ability to interfere with crucial biological pathways such as ribonucleotide reductase inhibition, topoisomerase II suppression, oxidative stress induction through reactive oxygen species generation, and interference with mitochondrial functions, which is further enhanced by the incorporation of various transition metals like copper, zinc, palladium, platinum, and iron, as these metals stabilize the ligand structure and augment their bioavailability, selectivity, and efficacy while minimizing off-target effects, with research restricted to September 2020 emphasizing that the structural diversity of thiosemicarbazones, achieved through ligand modifications such as the incorporation of heterocyclic moieties or hydrophobic groups, critically influences their biological activity by modulating metal coordination geometry, electronic properties, and lipophilicity, thereby optimizing their pharmacokinetics and pharmacodynamics, and their wide applicability in theoretical models, including docking studies and QSAR analyses, has provided valuable insights into their mechanism of action at the molecular level, with conceptual advancements focusing on their dual role as cytotoxic agents and enzyme inhibitors, making them promising candidates for the development of targeted therapeutic agents, while their ability to form stable complexes under physiological conditions has led to their evaluation as imaging agents and sensors in diagnostic applications, and the reviewed studies, sourced from comprehensive theoretical investigations and reviews indexed in established databases such as PubMed, Scopus, Web of Science, and Embase, collectively underscore the necessity for further refinement of synthetic strategies and ligand design to enhance their specificity and reduce potential toxicity, with the theoretical framework provided by quantum chemical calculations and molecular modeling offering a deeper understanding of their structure-activity relationships, highlighting the need for innovative approaches to translate these findings into clinical applications that leverage their unique coordination chemistry to address challenges in drug resistance and bioavailability in the future development of advanced thiosemicarbazone-based therapeutics.},
keywords = {Thiosemicarbazone complexes, Medicinal chemistry, Transition metal coordination, Pharmacological properties, Structure-activity relationships (SAR), Therapeutic agent development},
month = {May},
}