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Updated: Jul 6, 2025

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
FDA-approved heterocyclic molecules for cancer treatment: Synthesis, dosage, mechanism of action and their adverse
Mossaraf Hossain1, Imran Habib1, Koustav Singha1
1Synthetic Organic Research Laboratory, UGC-HRDC (Chemistry), University of North Bengal, Darjeeling, 734013, India.
Abstract:
As the incorporation of heterocycles increases the physical characteristics and biological activity of pharmacological molecules, heterocyclic scaffolds are commonly discovered as common cores in a wide spectrum of biologically active drugs. In the contemporary context, many heterocycles have arisen, playing vital roles in diverse pharmaceutical compounds that benefit humanity. Over 85 % of FDA-approved medication molecules contain heterocycles, and most importantly, numerous heterocyclic medicinal molecules indicate potential benefits against a range: of malignancies. The unique flexibility and dynamic core scaffold of these compounds have aided anticancer research. These medications are used to treat cancer patients by targeting particular genes, enzymes, and receptors. Aside from the drugs that are now on the market, numerous forms are being researched for their potential anti-cancer activity. Here in this review, we classified some molecules and biologically active heterocycles containing anticancer medicinal moieties approved by the FDA between 2019 and 2021 based on their use in various forms of cancer. We will focus on those that are suitable for cancer treatment, as well as the essential biochemical mechanisms of action, biological targets, synthetic methods, and inherent limiting considerations in their use.
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