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

dc.contributor.authorRatre, Pooja
dc.contributor.authorKulkarni, Swanand
dc.contributor.authorDas, Sweety
dc.contributor.authorLiang, Chengyuan
dc.contributor.authorMishra, Pradyumna Kumar
dc.contributor.authorThareja, Suresh
dc.date.accessioned2024-01-21T10:38:29Z
dc.date.accessioned2024-08-13T12:05:26Z
dc.date.available2024-01-21T10:38:29Z
dc.date.available2024-08-13T12:05:26Z
dc.date.issued2022-12-05T00:00:00
dc.description.abstractCoumarin is a bicyclic oxygen bearing heterocyclic scaffold formed by fusion of benzene with the pyrone ring. Because of its unique physicochemical characteristics and the ease with which it may be transformed into a wide range of functionalized coumarins during�synthesis, coumarin provides a privileged scaffold for medicinal chemists. As a result, many coumarin derivatives have been developed, synthesized, and evaluated to target a variety of therapeutic domains, thereby making it an attractive template for designing novel anti-breast cancer compounds. The main culprit in estrogen overproduction in the estrogen-dependent breast cancer (EDBC), is the enzyme aromatase (AR), and it is thought to be a significant target for the effective treatment of EDBC. Considering coumarins versatility, this review presents a detailed overview of diverse study of aromatase as a target for coumarins. An overview of structure�activity relationship analysis of coumarin core is also included so as to summarize the desired pharmacophoric features essential for design and development of aromatase inhibitors (AIs) using coumarin core. Identification of key synthesis techniques that could aid researchers in designing and developing novel analogues with significant anti-breast cancer properties along with their mechanism of action have also been covered in the current review. Graphical Abstract: [Figure not available: see fulltext.] � 2022, The Author(s), under exclusive licence to Springer Science+Business Media, LLC, part of Springer Nature.en_US
dc.identifier.doi10.1007/s12032-022-01916-4
dc.identifier.issn13570560
dc.identifier.urihttp://10.2.3.109/handle/32116/3584
dc.identifier.urlhttps://link.springer.com/10.1007/s12032-022-01916-4
dc.language.isoen_USen_US
dc.publisherSpringeren_US
dc.subjectAromataseen_US
dc.subjectAromatase inhibitorsen_US
dc.subjectBreast canceren_US
dc.subjectCoumarinen_US
dc.subjectSARen_US
dc.titleMedicinal chemistry aspects and synthetic strategies of coumarin as aromatase inhibitors: an overviewen_US
dc.title.journalMedical Oncologyen_US
dc.typeReviewen_US
dc.type.accesstypeClosed Accessen_US

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