Medicinal chemistry aspects and synthetic strategies of coumarin as aromatase inhibitors: an overview

Ratre, Pooja; Kulkarni, Swanand; Das, Sweety; Liang, Chengyuan; Mishra, Pradyumna Kumar; Thareja, Suresh

doi:10.1007/s12032-022-01916-4

Cited by 9 publications

(1 citation statement)

References 82 publications

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“…Here, we set out to create novel AR inhibitors with a coumarin ring as their active ingredient. One of the most potent aromatase inhibitors is a properly substituted coumarin derivative [40]. Compound 6 was selected because it showed the greatest in vitro aromatase inhibition efficacy when related to the reference blocker letrozole and the positive control cells.…”

Section: Aromatase Enzyme Assay Of Compoundmentioning

confidence: 99%

Novel 3-Substituted 8-Methoxycoumarin Derivatives as Anti-Breast Cancer Drugs

Al-Warhi,

Abu Ali,

Alqahtani

et al. 2023

Crystals

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Scientists have been interested in hybrid coumarin derivatives due to their wide clinical anticancer use. Herein, ethyl 8-methoxycoumarin-3-carboxylate (Compound 1) served as the starting material for the synthesis of a series of novel hybrid coumarin derivatives (Compounds 3–6). Their structure was determined using 13C NMR, 1H NMR, elemental analysis, and mass spectrometry. The in vitro cytotoxic activities of coumarin derivatives (Compounds 3, 5, and 6) and brominated coumarin derivatives (Compounds 4, 8, and 9) against MCF-7 and MDA-MB-231 were evaluated. Several substances have been identified as promising candidates for future study, especially Compound 6 due to its potent activity against β-tubulin (TUB) polymerization, sulfatase, and aromatase enzymes. It also has a role in inducing cell-cycle arrest at the S phase in the MCF-7 cell line, as well as apoptosis.

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Section: Aromatase Enzyme Assay Of Compoundmentioning

confidence: 99%