Design and Synthesis of New Aminothiazole-Benzazole Based Ureas: Antiproliferative and Antimigration Activity Studies


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Arslan G., Erzurumlu Y., Muhammed M. T., Özçelik A. B.

ChemistrySelect, cilt.9, sa.34, 2024 (SCI-Expanded, Scopus)

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 9 Sayı: 34
  • Basım Tarihi: 2024
  • Doi Numarası: 10.1002/slct.202402253
  • Dergi Adı: ChemistrySelect
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier
  • Anahtar Kelimeler: 1,3-Benzazol-2(3H)-one, 2-Amino-thiazole, Antimigration, Antiproliferative, Urea
  • Süleyman Demirel Üniversitesi Adresli: Evet

Özet

In our quest to develop new treatments for cancer, we synthesized and tested a series of urea-functionalized aminothiazole-benzazole analogs. Our primary focus was assessing their ability to inhibit the growth of breast cancer (MCF-7) and lung adenocarcinoma (A549) cells. Using 1H NMR, 13C NMR spectra, and high resolution mass spectrometry (HRMS), we confirmed the chemical structures of these compounds. Among them, compound 8a demonstrated significant cytotoxicity against MCF-7 cells, achieving an IC50 value of 9.6±0.6 μM. Similarly, compound 8e exhibited potent cytotoxicity against A549 cells, with an IC50 value of 9.2±1.1 μM. We further investigated the antimigration properties of all compounds that showed promising antiproliferative effects in both MCF-7 and A549 cells. Additionally, we evaluated how these compounds impact key apoptosis-related proteins: Caspase-7, PARP-1, BAX, and Bcl-2. These proteins play crucial roles in the regulation of programmed cell death. Overall, our findings suggest that these urea-functionalized aminothiazole-benzazole analogs hold promise as potential anticancer agents, warranting further exploration into their mechanisms of action and therapeutic potential.