Design and synthesis of aminothiazole-benzazole based amide: antiproliferative, antimigration activity and molecular docking studies

Arslan Karahan G. Erzurumlu Y. Muhammed M.T. Özçelik A.B.
February 2025 Springer

Medicinal Chemistry Research
2025 #34 Issue 2 406 - 422 pp.

In this study, we synthesized a series of amide-functionalized aminothiazole-benzazole analogs for potential application in cancer treatment. The chemical structures of these compounds were confirmed using proton nuclear magnetic resonance (¹H NMR), carbon-13 nuclear magnetic resonance (¹³C NMR) spectroscopy, and high-resolution mass spectrometry (HRMS). We evaluated the cytotoxicity of these compounds against breast cancer cells (MCF-7) and lung adenocarcinoma cells (A549). Notably, Compound 6b demonstrated significant cytotoxicity, with IC₅₀ values of 17.2 ± 1.9 μM for MCF-7 cells and 19.0 ± 3.2 μM for A549 cells. Furthermore, we assessed the antimigration properties of all synthesized compounds, observing promising antiproliferative effects in both MCF-7 and A549 cells. Compound 6b exhibited a significant antimigration effect, achieving a 50.2 ± 4.7% wound healing rate in MCF-7 cells. In addition, we examined the impact of these compounds on key apoptotic proteins, including Caspase-7, PARP-1, BAX, and Bcl-2, which are critical in the regulation of programmed cell death. The binding potentials of the active compounds to BAX and Bcl-2 were also supported by docking. Results that consolidate the in vitro study were obtained from the in silico analysis. Our results suggest that these amide-functionalized aminothiazole-benzazole analogs exhibit potential as anticancer agents and merit further investigation to elucidate their mechanisms of action and therapeutic potential.

1,3-benzazol-2(3H)-one , 2-aminothiazole , Amide , Antimigration , Antiproliferative

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Department of Biochemistry Faculty of Pharmacy, Suleyman Demirel University, Isparta, Kazakhstan
Department of Pharmaceutical Chemistry Faculty of Pharmacy, Gazi University, Ankara, Turkey
Department of Pharmaceutical Chemistry Faculty of Pharmacy, Suleyman Demirel University, Isparta, Kazakhstan

Department of Biochemistry Faculty of Pharmacy
Department of Pharmaceutical Chemistry Faculty of Pharmacy
Department of Pharmaceutical Chemistry Faculty of Pharmacy

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