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Paper | Regular issue | Vol 104, No. 5, 2022, pp.855-877
Published online, 16th February, 2022
DOI: 10.3987/COM-21-14535
Synthesis, Biological Evaluation, and In Silico Studies of New Heterocycles Incorporating 4,5,6,7-Tetrabromophthalimide Moiety as Potential Antibacterial and Anticancer Agents

Magda H. Abdellattif,* Hossam Nada, and Ahmed Elkamhawy

*Department of Chemistry, College of Science, Taif University, P.O. Box 11099, Taif, 21944, Saudi Arabia

Abstract

Cancer and infectious illnesses are currently the most significant public health issues in the globe. Phthalimide derivatives, including thalidomide (multi-target drug), have anti-inflammatory, analgesic, anticancer, antibacterial, and anticonvulsant biological activities. A new series of heterocyclic compounds incorporating 4,5,6,7-tetrabromophthalimide moiety were synthesized and biologically evaluated for potential antimicrobial and anticancer activities. While compounds 4ac and 11ac were the most active antimicrobial activities upon evaluation over Aspergillus favus, E. coli, Staphylococcus, and Fusarium moniliform, derivatives 4a and 4cb showed the most potent values over cervical and ovarian cancer (6.933‒11.46 µg/mL). Further in silico studies, including a molecular docking investigation over HSP90 protein, were carried out to investigate the potential binding mode and toxicity profile(s) of the newly synthesized compounds.