Bioactive Fluorenes. Part II. Unprecedented biologically active thiazole derivatives based-2,7-dichlorofluorene as competent DHFR inhibitors: Design, synthesis, and molecular docking approaches

Reem I. Alsantali, Essam M. Hussein, Rami J. Obaid, Moataz Morad, Hatem M. Altass, Ahmed Alharbi, Ahmed M. Hameed, Rabab S. Jassas, Mohamed A.S. Abourehab, Basim H. Asghar, Ziad Moussa, Saleh A. Ahmed

Research output: Contribution to journalArticlepeer-review

4 Citations (Scopus)

Abstract

In this study, a new series of (4-(2,7-dichloro-9H-fluoren-4-yl)thiazol-yl)acetamide derivatives was synthesized, and the new heterocycles were completely characterized, evaluated for their antimicrobial activity, and screened for cytotoxic activity against human lung carcinoma (A-549) and human breast carcinoma (MCF-7) cell lines. A molecular docking study was undertaken to identify the possible mode of action of the synthesized compounds, which suggested binding interactions with the dihydrofolate reductase (DHFR) active sites. Most of the synthesized compounds displayed meaningful activity against A-549 and MCF-7 cell lines when compared to 5-fluorouracil (5-FU), which was used as a reference drug. Furthermore, some of the prepared compounds exhibited potent antibacterial and antifungal activities. The highly pronounced biological activities of the compounds under investigation offer such species as promising future drug prospects which may find applications in the fields of biological and medicinal sciences.

Original languageEnglish
Pages (from-to)5451-5462
Number of pages12
JournalArabian Journal of Chemistry
Volume13
Issue number5
DOIs
Publication statusPublished - May 2020

Keywords

  • Anti-cancer
  • Antimicrobial
  • DHFR inhibitors
  • Fluorene
  • Molecular docking
  • Thiazole

ASJC Scopus subject areas

  • Chemistry(all)
  • Chemical Engineering(all)

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