Coumarin compounds represent an important type of naturally occurring and synthetic oxygen-containing heterocycles with typical benzopyrone framework. This type of special benzopyrone structure enables its derivatives readily interact with a diversity of enzymes and receptors in organisms through weak bond interactions, thereby exhibit wide potentiality as medicinal drugs. So far, some coumarin-based drugs such as anticoagulant and antineurodegenerative agents have been extensively used in clinic. Coumarin-containing supramolecular medicinal agents as a new increasing expansion of supramolecular chemistry in pharmaceutical science have also been actively investigated in recent years. Coumarin-derived artificial ion receptors, fluorescent probes and biological stains are growing quickly and have a variety of potential applications in monitoring timely enzyme activity, complex biological events as well as accurate pharmacological and pharmacokinetic properties. This review provides a systematic summary and insight of the whole range of medicinal chemistry in the current developments of coumarin compounds as anticoagulant, antineurodegenerative, anticancer, antioxidative, antibacterial, antifungal, antiviral, antiparasitic, antiinflammatory and analgesic, antidiabetic, antidepressive and other bioactive agents as well as supramolecular medicinal drugs, diagnostic agents and pathologic probes, and biological stains. Some rational design strategies, structure-activity relationships and action mechanisms are discussed. The perspectives of the future development of coumarinbased medicinal chemistry are also presented.

Current Developments of Coumarin Compounds in Medicinal Chemistry

Coumarins as anticancer agents: A review on synthetic strategies, mechanism of action and SAR studies

Recent applications of 1,3-thiazole core structure in the identification of new lead compounds and drug discovery.

4-Thiazolidinones: the advances continue….

Mannich bases in medicinal chemistry and drug design.

Synthesis and preliminary evaluation of some substituted coumarins as anticonvulsant agents.

New pyrazole derivatives: Synthesis, anti-inflammatory activity, cycloxygenase inhibition assay and evaluation of mPGES

New series of 6-substituted coumarin derivatives as effective factor Xa inhibitors: synthesis, in vivo antithrombotic evaluation and molecular docking.

Synthesis of substituted imidazo[2,1-b]-1,3,4-thiadiazoles 2a,b-6, substituted 1,3,4-thiadiazolo[3,2-a]pyrimidines 7- 9 and 1,3-disubstituted thioureas 10a-e was reported. Structures of all synthesized compounds were elucidated using IR, NMR and mass spectroscopy. All the prepared derivatives were evaluated for their cytotoxic activity against tumor cell line A549 (Non-Small Cell Lung Cancer Cell Line) using Sulfo-Rodamine B (SRB) standard method. Most of the tested compounds exhibited potent cytotoxicity especially compounds 4, 5, 8 and 10b-d (IC50 2.58-6.47 μM). In order to find a molecular target for newly synthesized compounds, docking study was performed to explore the possible binding mode of these compounds with the binding site of fibroblast stromelysin-1 enzyme, which is involved in several pathological conditions including cancer.

Synthesis of novel 1,3,4-thiadiazole analogues with expected anticancer activity

Synthesis of 2,5-disubstituted-1,3,4-oxadiazole (2a-c), 3-substituted aminomethyl-5-substituted-1,3,4-oxadiazole-2(3H)-thione (4a-m) and 2-substituted thio-5-substituted-1,3,4-oxadiazole (5a, b) had been described. All the synthesized derivatives were screened for anticancer activity against HT29 and MCF7 cancer cell lines using Sulfo-Rodamine B (SRB) standard method. Most of the tested compounds exploited potent antiproliferative activity against HT29 cancer cell line rather than MCF7 cancer cell line. Compounds 2a-c, 4f and 5a exhibited potent cytotoxicity (IC(50) 1.3-2.0 µM) and selectivity against HT29 cancer cell line. Quantitative structure-activity relationship (QSAR) study was applied to find a correlation between the experimental antiproliferative activities of the newly synthesized oxadiazole derivatives with their physicochemical parameter and topological index.

Synthesis, Quantitative Structure–Activity Relationship and Biological Evaluation of 1,3,4-Oxadiazole Derivatives Possessing Diphenylamine Moiety as Potential Anticancer Agents

Doaa E. Abdel Rahman

Papers

Synthesis and preliminary evaluation of some substituted coumarins as anticonvulsant agents.

New pyrazole derivatives: Synthesis, anti-inflammatory activity, cycloxygenase inhibition assay and evaluation of mPGES

New series of 6-substituted coumarin derivatives as effective factor Xa inhibitors: synthesis, in vivo antithrombotic evaluation and molecular docking.

Synthesis of novel 1,3,4-thiadiazole analogues with expected anticancer activity

Synthesis, Quantitative Structure–Activity Relationship and Biological Evaluation of 1,3,4-Oxadiazole Derivatives Possessing Diphenylamine Moiety as Potential Anticancer Agents