SYNTHESIS, BIOLOGICAL EVALUATION, AND IN SILICO STUDIES OF NEW HETEROCYCLES INCORPORATING 4,5,6,7-TETRABROMOPHTHALIMIDE MOIETY AS POTENTIAL ANTIBACTERIAL AND ANTICANCER AGENTS

  • Abdellattif, Magda H.
  • Nada, Hossam
  • Elkamhawy, Ahmed
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초록

??? 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 4a???c and 11a???c 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 ??g/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.

키워드

HSP90 MOLECULAR CHAPERONEDERIVATIVESVITROINHIBITORSCANCERDESIGNTARGET
제목
SYNTHESIS, BIOLOGICAL EVALUATION, AND IN SILICO STUDIES OF NEW HETEROCYCLES INCORPORATING 4,5,6,7-TETRABROMOPHTHALIMIDE MOIETY AS POTENTIAL ANTIBACTERIAL AND ANTICANCER AGENTS
저자
Abdellattif, Magda H.Nada, HossamElkamhawy, Ahmed
DOI
10.3987/COM-21-14535
발행일
2022-03
유형
Article
저널명
Heterocycles
104
5
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855 ~ 877