7th Eurasia Biochemical Approaches & Technologies (EBAT), Antalya, Türkiye, 6 - 09 Kasım 2025, ss.68, (Özet Bildiri)
Breast cancer is one of the most frequently diagnosed malignancies among women worldwide. The high toxicity and limited selectivity of conventional chemotherapeutic agents underscore the need for more effective and targeted therapeutic strategies.1 In this study, a series of quinazoline-based chiral thioureas (1a-f) were synthesized starting from natural amino acids L-alanine, L-valine, and L phenylalanine. The structures of the (1a-f) were determined by NMR, IR, and HRMS techniques, while their optical purities were confirmed through HPLC analysis. The antiproliferative activities of the synthesized chiral thioureas were evaluated against MCF-7 (breast cancer) and HT-29 (colon cancer) cell lines. Among the tested compounds, the L-alanine derived 1a exhibited the most potent cytotoxic effect against MCF-7 cells (IC₅₀ 0.65 µM), demonstrating stronger antiproliferative activity compared to carboplatin (7.77 µM) and docetaxel (12.65 µM). On the other hand, compound 1c exhibited the highest cytotoxic effect against the HT-29 cell line (IC₅₀ 30.10 µM). Notably, 1a demonstrates high cytotoxicity against cancer cells while potentially exerting minimal effects on healthy tissues. As a result, 1a represents a promising candidate for further preclinical evaluation, particularly in the context of MCF-7 breast cancer cells, due to its superior antiproliferative efficacy.