Design, Synthesis, and Evaluation of Benzoxazole-linked Pyrazole Hybrids as VEGFR-2-targeted Antiproliferative Agents

Deniz E., ÇÖVEN F. O., Ergüç A., Karakuş F., Kuzu B.

Cell Biochemistry and Biophysics, 2025 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Basım Tarihi: 2025
  • Doi Numarası: 10.1007/s12013-025-01817-z
  • Dergi Adı: Cell Biochemistry and Biophysics
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, BIOSIS, Biotechnology Research Abstracts, Chemical Abstracts Core, EMBASE, MEDLINE
  • Anahtar Kelimeler: Antiproliferation, Benzoxazole, Molecular docking, Pyrazole, VEGFR-2
  • Van Yüzüncü Yıl Üniversitesi Adresli: Evet

Özet

In this study, a series of benzoxazole-linked pyrazole compounds (20a–t) were synthesized and tested for their antiproliferative activity. Their effects on lung cancer (A549) and normal lung (CCD-34Lu) cell lines were evaluated using the MTT assay. Among them, compounds 20m and o showed strong antiproliferative effects, with IC50 values of 7.64 and 15.82 µM, respectively, and selectivity indices of 2.84 and 1.95 in favor of cancer cells. ELISA tests demonstrated that both compounds statistically significantly reduced VEGFR-2 protein levels by 24.8 and 28.7% at their respective IC50 values, indicating potential antiangiogenic properties. Molecular docking studies supported these findings by showing favorable binding of 20m and o to the VEGFR-2 receptor, with binding energies of −7.33 kcal/mol and −7.22 kcal/mol, respectively. Overall, compounds 20m and o stand out as promising candidates for further development as anticancer drugs.