Research Article

Design and Synthesis of Imidazole Derivatives as Anticancer Agents and Potential Aromatase Inhibitors

Volume: 43 Number: 4 December 27, 2022
EN

Design and Synthesis of Imidazole Derivatives as Anticancer Agents and Potential Aromatase Inhibitors

Abstract

In this study, imidazole derivative compounds were synthesized using the Debus-Radziszewski method. The chemical structures of the compounds were characterized by spectroscopic methods. The effects of target compounds on MCF7 (CRL-3435) were examined and their IC50 values and percent viability were calculated. In addition, the cytotoxic effects on the L929 (CCL-1) normal cell line were evaluated in order to determine the selectivities of the compounds. Then, the inhibition values of aromatase enzyme of the compounds were calculated and compared to the reference compound. When the results were examined, it was observed that Compound la caused the death of breast cancer cells, although not as much as cisplatin, but did not harm healthy cells. In this respect, it was determined that compound Ia has a promising anticancer effect as an aromatase inhibitor.

Keywords

References

  1. [1] Lekgau K., Raphoko L.A., Lebepe C.M., Mongokoana D.F., Leboho T.C., Matsebatlela T. M., ... & Nxumalo W., Design and Synthesis of 6-Amino-quinoxaline-alkynyl as Potential Aromatase (CYP19A1) Inhibitors, J. Mol. Struct., 1255 (2022) 132473.
  2. [2] Osmaniye D., Karaca Ş., Kurban B., Baysal M., Ahmad I., Patel H., ... Kaplancıklı Z. A., Design, synthesis, molecular docking and molecular dynamics studies of novel triazolothiadiazine derivatives containing furan or thiophene rings as anticancer agents, Bioorg. Chem., 122 (2022) 105709.
  3. [3] Sayyad N. B., Sabale P. M., Umare M. D., Bajaj K. K., (2022). Aromatase Inhibitors: Development and Current Perspectives, Indian J. Pharm. Educ. Res.56 (2022) 311-320.
  4. [4] Shah V., Bhaliya J., Patel G. M., In silico docking and ADME study of deketene curcumin derivatives (DKC) as an aromatase inhibitor or antagonist to the estrogen-alpha positive receptor (Erα+): potent application of breast cancer, Struct. Chem., 33 (2022) 571-600.
  5. [5] Rashdan H. R., Shehadi I. A., Triazoles Synthesis & Applications as Nonsteroidal Aromatase Inhibitors for Hormone-Dependent Breast Cancer Treatment, Heteroatom Chem., (2022).
  6. [6] Çevik U. A., Celik I., Mella J., Mellado M., Özkay Y., Kaplancıklı Z. A., Design, Synthesis, and Molecular Modeling Studies of a Novel Benzimidazole as an Aromatase Inhibitor, ACS omega. 7 (2022) 16152-16163.
  7. [7] Osmaniye D., Levent S., Sağlık B. N., Karaduman A. B., Özkay Y., Kaplancıklı Z. A., Novel imidazole derivatives as potential aromatase and monoamine oxidase-B inhibitors against breast cancer, New J. Chem., 46 (2022) 7442-7451.
  8. [8] Ammazzalorso A., Gallorini M., Fantacuzzi M., Gambacorta N., De Filippis B., Giampietro L., ... Amoroso R., Design, synthesis and biological evaluation of imidazole and triazole-based carbamates as novel aromatase inhibitors, Eur. J. Med. Chem., 211 (2021) 113115.

Details

Primary Language

English

Subjects

Pharmacology and Pharmaceutical Sciences

Journal Section

Research Article

Publication Date

December 27, 2022

Submission Date

June 15, 2022

Acceptance Date

September 28, 2022

Published in Issue

Year 2022 Volume: 43 Number: 4

APA
Bostancı, H. E., & Acar Çevik, U. (2022). Design and Synthesis of Imidazole Derivatives as Anticancer Agents and Potential Aromatase Inhibitors. Cumhuriyet Science Journal, 43(4), 590-593. https://doi.org/10.17776/csj.1131485

As of 2026, Cumhuriyet Science Journal will be published in six issues per year, released in February, April, June, August, October, and December