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

Arabian Journal of Chemistry

Moataz Morad¹  Hatem M. Altass²  Essam M. Hussein³  Reem I. Alsantali⁴  Mohamed A.S. Abourehab⁴  Rabab.S. Jassas⁴  Ahmed Alharbi⁴  Basim H. Asghar⁴  Rami J. Obaid⁴  Ahmed M. Hameed⁴  Ziad Moussa⁵  Saleh A. Ahmed⁶ 

[1] Chemistry Department, Faculty of Science, Assiut University, 71516 Assiut, Egypt;Corresponding authors at: Department of Chemistry, Faculty of Applied Science, Umm Al-Qura University, 21955 Makkah, Saudi Arabia. Tel./Fax: + 966 530435760 (E.M. Hussein);Department of Pharmaceutical Chemistry, Pharmacy College, Taif University, 888 Taif, Saudi Arabia;Department of Chemistry, Faculty of Applied Science, Umm Al-Qura University, 21955 Makkah, Saudi Arabia;Department of Chemistry, Jamoum University College, Umm Al-Qura University, 21955 Makkah, Saudi Arabia;Department of Pharmaceutics, Faculty of Pharmacy, Umm Al-Qura University, Makkah, Saudi Arabia;

关键词: Fluorene;    Thiazole;    Antimicrobial;    Anti-cancer;    Molecular docking;    DHFR inhibitors;   

DOI  :  

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown