Atatürk Üniversitesi Atatürk Üniversitesi
Ara
Yayınlara dön
Makale Tam Makale Uluslararası 2020

Design, synthesis and biological evaluation of 3,5-diaryl isoxazole derivatives as potential anticancer agents

Derya Anıl, Gökçen Akinalp, Fatma Sanli, Mehmet Ali Yucel, Nicola Gambacorta, Orazio Nicolotti, Omer Faruk Karatas, Oztekin Algul, Serdar Burmaoğlu

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS Cilt 30 · 01.10.2020
DOI ile aç

Özet

The present study was carried out in the attempt to synthesize a new class of potential anticancer agents comprising eleven compounds (24-34) sharing the 3,5-diarylisoxazole as a core. The chemical structure of the new synthesized compounds was established by IR, H-1 NMR, C-13 NMR and elemental analysis. Their biological potential towards prostate cancer was evaluated by using cancer PC3 cells and non-tumorigenic PNT1a cells. Interestingly, compound 26 distinguished from others with a quite high selectivity value that is comparable to 5-FU. The binding mode of 26 towards Ribosomal protein S6 kinase beta-1 (S6K1) was investigated at a molecular level of detail by employing docking simulations based on GLIDE standard precision as well as MM-GBSA calculations.

Anahtar kelimeler

EXPRESSION PROLIFERATION INHIBITION apoptosis Synthesis molecular modeling PROSTATE-CANCER isoxazole anticancer agent SUPPRESSION CYTOCHROME-P450 1B1

Sürdürülebilir Kalkınma Amaçları

  • SKA 3: Sağlıklı Bireyler

Atıf için künye

Anıl, D., Akinalp, G., Sanli, F., Yucel, M. A., Gambacorta, N., Nicolotti, O., Karatas, O. F., Algul, O., & Burmaoğlu, S. (2020). Design, synthesis and biological evaluation of 3,5-diaryl isoxazole derivatives as potential anticancer agents. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 30. https://doi.org/10.1016/j.bmcl.2020.127427

BibTeX
@article{anil2020-78349,
  author = {Anıl, Derya and Akinalp, Gökçen and Sanli, Fatma and Yucel, Mehmet Ali and Gambacorta, Nicola and Nicolotti, Orazio and Karatas, Omer Faruk and Algul, Oztekin and Burmaoğlu, Serdar},
  title = {Design, synthesis and biological evaluation of 3,5-diaryl isoxazole derivatives as potential anticancer agents},
  journal = {BIOORGANIC & MEDICINAL CHEMISTRY LETTERS},
  year = {2020},
  volume = {30},
  issn = {0960-894X},
  doi = {10.1016/j.bmcl.2020.127427},
  url = {https://akademik.atauni.edu.tr/yayinlar/78349-design-synthesis-and-biological-evaluation-of-35-diaryl-isoxazole-derivatives-as}
}