Bioactive fluorenes. part I. Synthesis, pharmacological study and molecular docking of novel dihydrofolate reductase inhibitors based-2, 7-dichlorofluorene. Issue 6 (June 2019)

• Record Type: Journal Article
• Authors: Hussein, Essam M.; Alsantali, Reem I.; Abd El-Galil, Shimaa M.; Obaid, Rami J.; Alharbi, Ahmed; Abourehab, Mohamed A.S.; Ahmed, Saleh A.
• Is Part Of: Heliyon. Volume 5:Issue 6(2019)
• Publication Date: 2019-06
• Subjects: Organic chemistry -- Fluorene -- Anti-cancer -- Antimicrobial -- DHFR inhibitors -- Molecular docking; Research -- Periodicals; Medical sciences -- Periodicals; Natural history -- Periodicals; Social sciences -- Periodicals; Earth sciences -- Periodicals; Physical sciences -- Periodicals; 507.2
• DOI: 10.1016/j.heliyon.2019.e01982
• Languages: English
• ISSNs: 2405-8440

Abstract

Abstract: In this study, a new series of 2, 7-dichloro-4-(2-substituted-amino acetyl)fluorene derivatives were synthesized, characterized and evaluated for their antimicrobial activity and screened for cytotoxic activity against human lung carcinoma (A-549) and human breast carcinoma (MCF-7) cell lines. Most of the synthesized compounds displayed significant activity against A-549 and MCF-7 cell lines when compared to 5-fluorouracil (5-FU), which was used as a reference drug. In addition, some of these reported novel compounds exhibited promising antibacterial and antifungal properties. A molecular docking study was performed to identify the mechanism of action of the synthesized compounds, which suggested binding interactions with the active sites of dihydrofolate reductase (DHFR).