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Structural diversity, pharmacological relevance, and the ability to include N-containing heterocyclic derivatives through medicinal chemistry make these heterocyclic compounds known as essential scaffolds for the design and development of anticancer agents. Uncontrolled cell proliferation with metastasis remains a leading cause of global mortality from cancer. Enzyme binding sites interact with compounds with N-heterocycle to inhibit critical processes in cancer cells. The relative ease of synthesis, selective penetration, and low toxicity of these compounds make them desirable for use as a source of new therapeutic discoveries (over 90% of new therapeutic discoveries with approximately 65% of FDA-approved anticancer drugs (2010-2015). Focusing on selectivity, bioavailability, and low toxicity, this article compares the latest advancements in anticancer drug discovery, emphasizing the significance of SAR analysis in enhancing potency, efficacy, and development of N-heterocycle-based anticancer agents to overcome drug resistance.
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