Design, Synthesis, and Evaluation of Pyrrolopyrazine-Substituted Benzoxazole/Benzothiazole Derivatives Targeting Aurora Kinase A in MCF-7 Cells
ChemistrySelect, cilt.10, sa.22, 2025 (SCI-Expanded, Scopus)
- Yayın Türü: Makale / Tam Makale
- Cilt numarası: 10 Sayı: 22
- Basım Tarihi: 2025
- Doi Numarası: 10.1002/slct.202502066
- Dergi Adı: ChemistrySelect
- Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier
- Anahtar Kelimeler: Antiproliferation, AURKA, Benzothiazole, Benzoxazole, Pyrrolopyrazine
- Van Yüzüncü Yıl Üniversitesi Adresli: Evet
Özet
This study reports the synthesis, characterization, and biological evaluation of 19 benzoxazole/benzothiazole hybrids (19a-s). The compounds were synthesized through a multi-step process and structurally confirmed via NMR, elemental, and MS analyzes. Their antiproliferative effects were assessed on MCF-7 breast cancer and HME1 healthy epithelial cells. MTT assays identified 15 compounds with significant cytotoxic activity, among which 19e, 19g, 19i, 19j, and 19k exhibited high selectivity for MCF-7 cells. ELISA results demonstrated that 19g, 19i, 19j, and 19k significantly reduced AURKA protein levels in MCF-7 cells, while sparing healthy cells, suggesting their role in inhibiting cancer cell proliferation. These findings highlight 19g, 19i, 19j, and 19k as promising selective AURKA-targeted agents for breast cancer therapy.