Design and Synthesis of Novel Triazole-based Peptide Analogues as Anticancer Agents

Area of Science:

• Medicinal Chemistry
• Peptide Chemistry
• Oncology

Background:

• Cancer remains a significant global health challenge with unmet therapeutic needs.
• Anticancer peptides (ACPs) are emerging as promising drug candidates due to their favorable properties like high activity and biocompatibility.
• Developing novel ACPs with enhanced efficacy and safety is crucial for advancing cancer treatment.

Purpose of the Study:

• To synthesize novel triazole-based analogues incorporating a peptide scaffold.
• To evaluate the in vitro anticancer activities of these compounds against breast and colon cancer cell lines.
• To explore the potential of these peptide analogues as new anticancer agents.

Main Methods:

• Synthesis of triazole-based analogues using click chemistry.
• Evaluation of cytotoxicity using the MTT assay.
• Testing against human breast (MDA-MB-231, MCF-7) and colon cancer cell lines, and fibroblast cells.

Main Results:

• The synthesized peptide analogues containing 1H-1,2,3-triazole rings exhibited significant toxicity against colon and breast cancer cells.
• The compounds showed more pronounced toxicity against MDA-MB-231 (breast cancer) cells compared to MCF-7 (breast cancer) cells.
• Fibroblast cells were used as a control to assess selectivity, indicating potential safety.

Conclusions:

• The designed triazole-based peptide analogues possess potent anticancer properties.
• These compounds demonstrate selective toxicity towards cancer cells, suggesting a favorable safety profile.
• The novel peptide analogues represent promising candidates for the development of future anticancer therapeutics.