Bioactive Fluorenes. Part I. Synthesis, Pharmacological Study and Molecular Docking of Novel Dihydrofolate Reductase Inhibitors Based-2,7-dichlorofluorene

Overview

Journal Heliyon

Specialty Social Sciences

Date 2019 Jul 16

PMID 31304415

Citations 7

Authors

Essam M Hussein

Reem I Alsantali

Shimaa M Abd El-Galil

Rami J Obaid

Ahmed Alharbi

Mohamed A S Abourehab

Saleh A Ahmed

Affiliations

Soon will be listed here.

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).

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