Synthesis of diaryl urea derivatives and evaluation of their antiproliferative activities in colon adenocarcinoma


GÖMEÇ M., YULAK F., GEZEGEN H., ÖZKARACA M., SAYIN K., ATASEVEN H.

JOURNAL OF MOLECULAR STRUCTURE, vol.1254, 2022 (Peer-Reviewed Journal) identifier identifier

  • Publication Type: Article / Article
  • Volume: 1254
  • Publication Date: 2022
  • Doi Number: 10.1016/j.molstruc.2021.132318
  • Journal Name: JOURNAL OF MOLECULAR STRUCTURE
  • Journal Indexes: Science Citation Index Expanded, Scopus, Academic Search Premier, Chimica, Compendex, INSPEC
  • Keywords: Synthesis, Anticancer, Colon cancer, Diaryl urea, In silico, SULFONYLUREA DERIVATIVES, AUTOPHAGY, CANCER, INHIBITION, APOPTOSIS, RESECTION, DAMAGE, CELLS

Abstract

Colon cancer is one of the leading causes of cancer-related deaths today. Serious research for ideal chemotherapy continues today. In this context, newly synthesized molecules have an essential role in cancer treatment research. The effects of 5 diaryl urea derivatives synthesized within the scope of this study on the HT-29 colon cancer cell line were investigated for the first time in the literature by in-silico and in-vitro methods. Among the five compounds produced in the first stage of the study, DAU5 was found to have a cytotoxic effect on HT-29. However, it was determined that it did not show a serious cytotoxic effect on L929 (healthy fibroblast cell line) at the same doses. The efficacy of DAU5 was evaluated for expression of LC3B, an indicator of autophagy, and 8-OHdG, an indicator of oxidative stress-DNA damage. LC3B and 8-OHdG expression were lower in the DAU5 treatment group than in the control group. As a result, it was seen that DAU5, a diaryl urea derivative compound we synthesized in this study, has the potential to be a chemotherapeutic agent against colon cancer. However, our study needs to be supported by in vivo and clinical studies. (C) 2022 Elsevier B.V. All rights reserved.