Design, Synthesis, and Evaluation of Pyrrolopyrazine-Substituted Benzoxazole/Benzothiazole Derivatives Targeting Aurora Kinase A in MCF-7 Cells

Kuzu B., Köstekci S., Karakuş F., Tülüce Y.

ChemistrySelect, cilt.10, sa.22, 2025 (SCI-Expanded) identifier

  • 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.