Bioactive fluorenes. part I. Synthesis, pharmacological study and molecular docking of novel dihydrofolate reductase inhibitors based-2,7-dichlorofluorene

生物活性芴化合物I.基于2,7-二氯芴的新型二氢叶酸还原酶抑制剂的合成、药理研究及分子对接

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作者:Essam M Hussein, Reem I Alsantali, Shimaa M Abd El-Galil, Rami J Obaid, Ahmed Alharbi, Mohamed A S Abourehab, Saleh A Ahmed

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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