Mini review highlights advancements in anti-EGFR pyrazoline derivatives, suggesting improved efficacy and reduced toxicity.
Pyrazoline and its derivatives continue to be widely used heterocycles in drug development and design. The scientific community has studied pyrazoline derivatives in detail due to their wide range of biological activity, particularly their anti-EGFR properties. Since EGFR dysfunction has been linked to several cancers, overexpression of EGFR signalling promotes tumour growth by inhibiting apoptosis. As a result, EGFR represents a potential target for cancer treatment. Many anti-EGFR drugs are on the market, including dacomitinib, erlotinib, and afatinib. However, nearly all these medications have limited therapeutic efficacy because of their lack of selectivity and significant side effects. New and effective anti-EGFR therapeutics with little toxicity is required to address this. Pyrazoline derivatives have been studied as a potential pharmacophore for creating novel drugs with improved efficacy, reduced toxicity, and desired pharmacokinetic characteristics to counteract therapeutic resistance to EGFR inhibitors. Five years of progress toward EGFR-blocking pyrazoline-based compound research are summarized in the current review.
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Bhendarkar et al. (2025) studied this question.
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