TY - JOUR
T1 - SYNTHESIS, BIOLOGICAL EVALUATION, AND IN SILICO STUDIES OF NEW HETEROCYCLES INCORPORATING 4,5,6,7-TETRABROMOPHTHALIMIDE MOIETY AS POTENTIAL ANTIBACTERIAL AND ANTICANCER AGENTS
AU - Abdellattif, Magda H.
AU - Nada, Hossam
AU - Elkamhawy, Ahmed
N1 - Publisher Copyright:
© 2022 Japan Institute of Heterocyclic Chemistry. All rights reserved.
PY - 2022
Y1 - 2022
N2 - 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 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 profiles(s) of the newly synthesized compounds.
AB - 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 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 profiles(s) of the newly synthesized compounds.
UR - http://www.scopus.com/inward/record.url?scp=85125860947&partnerID=8YFLogxK
U2 - 10.3987/COM-21-14535
DO - 10.3987/COM-21-14535
M3 - Article
AN - SCOPUS:85125860947
SN - 0385-5414
VL - 104
JO - Heterocycles
JF - Heterocycles
IS - 5
ER -