Novel thiazoline–coumarin hybrid compounds containing sugar moieties: synthesis, biological evaluation and molecular docking study as antiproliferative agents

Abstract

A new series of 2,3-4-thiazoline−coumarin hybrid compounds that contained D-glucose and D-galactose moieties (4a-g) were synthesized and evaluated their cytotoxic activity against breast adenocarcinoma (MCF-7), human liver cancer (HepG2), human...

Coumarin as an Elite Scaffold in Anti-Breast Cancer Drug Development: Design Strategies, Mechanistic Insights, and Structure–Activity Relationships

“…The results of the assay demonstrated that compound 56 , with an IC 50 value of 1.91 µM against the MCF-7 cell line, was the most potent compound in the series. The structure–activity relationship revealed that the substitution of the alkyl chain up to five carbons on the coumarin via an ether linkage was beneficial for the activity of the compound, whereas with the decrease in the length of the chain, the activity decreased ( Figure 18 ) [ 145 ].…”

Design, Synthesis and Cytotoxicity of New Coumarin‐1,2,3‐triazole Derivatives: Evaluation of Anticancer Activity and Molecular Docking Studies

“…[9,10] The coumarin molecules are familiar and notorious moities with several applications, and vital action is occurring in arrears to concession of shape and physicochemical properties of the 2-benzopyrone entity. [11][12][13][14] However, coumarin and its derivatives were found to have a wide range of biological and pharmaceutical activities and have been used as good activity agents over decades for the cure of cancer and HIV, [15] coagulant, [16] oxidant [17] and inflammatory [18] and also used as the fascinating aspects to control or to heal of asthma and arthritis. [19] The synthesized derivatives of coumarin and Dgalactose moieties reports of Toan and coauthors showed worthy of action against EGFRÀ L858R and EGFRÀ T790 M tyrosine kinase.…”