Rational approaches, design strategies, structure activity relationship and mechanistic insights for therapeutic coumarin hybrids Review


Authors: Singh, H.; Singh, J. V.; Bhagat, K.; Gulati, H. K.; Sanduja, M.; Kumar, N.; Kinarivala, N.; Sharma, S.
Review Title: Rational approaches, design strategies, structure activity relationship and mechanistic insights for therapeutic coumarin hybrids
Abstract: Hybrid molecules, furnished by combining two or more pharmacophores is an emerging concept in the field of medicinal chemistry and drug discovery that has attracted substantial traction in the past few years. Naturally occurring scaffolds such as coumarins display a wide spectrum of pharmacological activities including anticancer, antibiotic, antidiabetic and others, by acting on multiple targets. In this view, various coumarin-based hybrids possessing diverse medicinal attributes were synthesized in the last five years by conjugating coumarin moiety with other therapeutic pharmacophores. The current review summarizes the recent development (2014 and onwards) of these pharmacologically active coumarin hybrids and demonstrates rationale behind their design, structure-activity relationships (SAR) and mechanistic studies performed on these hybrid molecules. This review will be beneficial for medicinal chemist and chemical biologist, and in general to the drug discovery community and will facilitate the synthesis and development of novel, potent coumarin hybrid molecules serving as lead molecules for the treatment of complex disorders. © 2019 Elsevier Ltd
Keywords: structure-activity relationship; antioxidant; mechanistic insights; anticancer; anti-inflammatory; antimicrobial; anti-alzheimer's; antidiabetic; coumarin hybrids; design strategies
Journal Title: Bioorganic & Medicinal Chemistry
Volume: 27
Issue: 16
ISSN: 0968-0896
Publisher: Pergamon-Elsevier Science Ltd  
Date Published: 2019-08-15
Start Page: 3477
End Page: 3510
Language: English
DOI: 10.1016/j.bmc.2019.06.033
PUBMED: 31255497
PROVIDER: scopus
PMCID: PMC7970831
DOI/URL:
Notes: Source: Scopus
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  1. Sahil Sharma
    31 Sharma
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