Pharmacological Evaluation of Bioisosterically Replaced and Triazole- Tethered Derivatives for Anticancer Therapy

Area of Science:

• Medicinal Chemistry
• Pharmacology
• Organic Chemistry

Background:

• Cancer remains a leading cause of mortality globally, with current therapies facing challenges like toxicity and drug resistance.
• There is a critical need for novel anticancer agents with improved efficacy and safety profiles.
• Triazole moieties offer a promising scaffold for developing new hybrid anticancer drugs.

Purpose of the Study:

• To review recent advancements in triazole-based anticancer agents.
• To analyze the chemical structures, mechanisms of action, and structure-activity relationships of these compounds.
• To highlight clinical and nonclinical trials of triazole-derived hybrid drugs.

Main Methods:

• Literature review of articles published from the early 2000s to the 2020s.
• Analysis of chemical structures and integration strategies of triazole moieties.
• Examination of target receptors/enzymes and mechanisms of action.
• Evaluation of structure-activity relationships and clinical trial data.

Main Results:

• Triazole incorporation via bioisosteric replacement, click chemistry, and organocatalysis yields potent anticancer pharmacophores.
• Numerous triazole-based derivatives exhibit promising anticancer activity against various cancer types.
• Several hybrid drugs are progressing through clinical and nonclinical trials, demonstrating therapeutic potential.

Conclusions:

• Triazole-based hybrid drugs represent a significant advancement in anticancer therapy development.
• These novel agents offer a promising strategy to overcome limitations of existing treatments, including reduced toxicity and enhanced potency.
• Continued research into triazole derivatives is crucial for developing next-generation cancer therapeutics.