Synthesis and Biological Evaluation of Novel Paracetamol-Triazole Conjugates


KULABAŞ N., GÜRBOĞA M., Özakpinar Ö. B., Liu J., Jakobsson P., DANIŞ Ö., ...Daha Fazla

Fabad Journal of Pharmaceutical Sciences, cilt.48, sa.3, ss.395-410, 2023 (Scopus) identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 48 Sayı: 3
  • Basım Tarihi: 2023
  • Doi Numarası: 10.55262/fabadeczacilik.1336831
  • Dergi Adı: Fabad Journal of Pharmaceutical Sciences
  • Derginin Tarandığı İndeksler: Scopus, EMBASE, International Pharmaceutical Abstracts, TR DİZİN (ULAKBİM)
  • Sayfa Sayıları: ss.395-410
  • Anahtar Kelimeler: 1,2,4-triazole, cancer, COX-1/2, mPGES-1, Paracetamol
  • Marmara Üniversitesi Adresli: Evet

Özet

Some new triazole containing acetamide derivatives 9-20 using paracetamol as starting material were synthesized, and their structures were verified by FTIR, NMR (1H and 13C) and mass spectral data. Compounds 9-20 were tested against five human cancer cell lines (lung cancer A549, chronic myelogenous leukemia K562, breast cancer MCF-7, prostate cancer PC-3, neuroblastoma SH-SY5Y cell lines) for in vitro cytotoxic activities. They were also evaluated their cytotoxic effect on mouse embryonic fibroblast cells (NIH/3T3) to define selectivity by MTT assay. Additionally, we evaluated the potential mPGES-1 and COX-1/2 inhibitory effect of twelve target compounds 9-20. While none of the synthesized compounds exhibited significant inhibition against both cancer cells and mPGES-1 as well as COX-1/2, it was determined that they were not cytotoxic against healthy cells, too. Finally, ADMET properties of newly synthesized compounds were estimated using in silico methods.