Design, synthesis, biological evaluation, and docking studies of novel (imidazol-5-yl)pyrimidine-based derivatives as dual BRAFV600E/p38α inhibitors
Journal Article
Ali, E. M., El-Telbany, R. F. A., Abdel-Maksoud, M. S., Ammar, U. M., Mersal, K. I., Zaraei, S., …Oh, C. (2021)
Design, synthesis, biological evaluation, and docking studies of novel (imidazol-5-yl)pyrimidine-based derivatives as dual BRAFV600E/p38α inhibitors. European Journal of Medicinal Chemistry, 215, Article 113277. https://doi.org/10.1016/j.ejmech.2021.113277
The synergistic effect of dual inhibition of serine/threonine protein kinases that are involved in the same signalling pathway of the diseases can exert superior biological be...
Design, synthesis and anti-inflammatory activity of imidazol-5-yl pyridine derivatives as p38α/MAPK14 inhibitor
Journal Article
Ali, E. M., Abdel-Maksoud, M. S., Hassan, R. M., Mersal, K. I., Ammar, U. M., Se-In, C., …Oh, C. (2021)
Design, synthesis and anti-inflammatory activity of imidazol-5-yl pyridine derivatives as p38α/MAPK14 inhibitor. Bioorganic and Medicinal Chemistry, 31, Article 115969. https://doi.org/10.1016/j.bmc.2020.115969
P38α/MAPK14 is intracellular signalling regulator involved in biosynthesis of inflammatory mediator cytokines (TNF-α, IL-1, IL-6, and IL-1b), which induce the production of in...
Design, synthesis, and biological evaluation of novel imidazole derivatives possessing terminal sulphonamides as potential BRAFV600E inhibitors
Journal Article
Ali, E. M., Abdel-Maksoud, M. S., Ammar, U. M., Mersal, K. I., Ho Yoo, K., Jooryeong, P., & Oh, C. (2021)
Design, synthesis, and biological evaluation of novel imidazole derivatives possessing terminal sulphonamides as potential BRAFV600E inhibitors. Bioorganic Chemistry, 106, Article 104508. https://doi.org/10.1016/j.bioorg.2020.104508
BRAF V600E mutation has been detected in various malignant tumours. Developing of potent BRAF V600E inhibitors is considered a leading step in the way to cure different cancer...
Design, synthesis, and anticancer activity of imidazo[2,1-b]oxazole-based RAF kinase inhibitors
Journal Article
Abdel-Maksoud, M. S., Ammar, U. M., El-Gamal, M. I., Gamal El-Din, M. M., Mersal, K. I., Ali, E. M., …Oh, C. (2019)
Design, synthesis, and anticancer activity of imidazo[2,1-b]oxazole-based RAF kinase inhibitors. Bioorganic Chemistry, 93, Article 103349. https://doi.org/10.1016/j.bioorg.2019.103349
In the present work, a novel series of B-RAF kinase inhibitors having imidazo[2,1-b]oxazole scaffold was designed and synthesized based on the structures of the well-known B-R...
Design and synthesis of novel pyrrolo[2,3-b]pyridine derivatives targeting V600EBRAF
Journal Article
Abdel-Maksoud, M. S., Ali, E. M., Ammar, U. M., Mersal, K. I., Yoo, K. H., & Oh, C. (2020)
Design and synthesis of novel pyrrolo[2,3-b]pyridine derivatives targeting V600EBRAF. Bioorganic and Medicinal Chemistry, 28(11), Article 115493. https://doi.org/10.1016/j.bmc.2020.115493
Several pyrrolo[2,3-b]pyridine-based B-RAF inhibitors are well known and some of them are currently FDA approved as anticancer agents. Based on the structure of these FDA appr...
Anticancer profile of newly synthesized BRAF inhibitors possess 5-(pyrimidin-4-yl)imidazo[2,1-b]thiazole scaffold
Journal Article
Abdel-Maksoud, M. S., Ammar, U. M., & Oh, C. (2019)
Anticancer profile of newly synthesized BRAF inhibitors possess 5-(pyrimidin-4-yl)imidazo[2,1-b]thiazole scaffold. Bioorganic and Medicinal Chemistry, 27(10), 2041-2051. https://doi.org/10.1016/j.bmc.2019.03.062
In this work, a new series of imidazo[2,1-b]thiazole was designed and synthesized. The new compounds are having 3-fluorophenyl at position 6 of imidazo[2,1-b]thiazole and pyri...
Recent advances of RAF (rapidly accelerated fibrosarcoma) inhibitors as anti-cancer agents
Journal Article
Ammar, U. M., Abdel-Maksoud, M. S., & Oh, C. (2018)
Recent advances of RAF (rapidly accelerated fibrosarcoma) inhibitors as anti-cancer agents. European Journal of Medicinal Chemistry, 158, 144-166. https://doi.org/10.1016/j.ejmech.2018.09.005
Frequent oncogenic mutations have been identified in MAPK (mitogen-activated protein kinase) signaling pathway components. As a result, MAPK pathway is associated with human c...
Design, synthesis, in vitro determination and molecular docking studies of 4-(1-(tert-butyl)-3-phenyl-1H-pyrazol-4-yl) pyridine derivatives with terminal sulfonamide derivatives in LPS-induced RAW264.7 macrophage cells
Journal Article
Mersal, K. I., Abdel-Maksoud, M. S., Ali, E. M. H., Ammar, U. M., Zaraei, S., Kim, J., …Oh, C. (2021)
Design, synthesis, in vitro determination and molecular docking studies of 4-(1-(tert-butyl)-3-phenyl-1H-pyrazol-4-yl) pyridine derivatives with terminal sulfonamide derivatives in LPS-induced RAW264.7 macrophage cells. Medicinal Chemistry Research, 30, 1925-1942. https://doi.org/10.1007/s00044-021-02784-9
In the present work, a new series of 4-(1-(tert-butyl)-3-phenyl-1H-pyrazol-4-yl) pyridine possessing terminal ethyl or propyl sulfonamides was designed and synthesized. The cy...
Design, synthesis, anticancer evaluation and molecular docking of new V600EBRAF inhibitors derived from pyridopyrazinone
Journal Article
Amin, K., El-Badry, O., Abdel Rahman, D., Ammar, U., & Abdalla, M. (2016)
Design, synthesis, anticancer evaluation and molecular docking of new V600EBRAF inhibitors derived from pyridopyrazinone. European Journal of Chemistry, 7(1), 19-29. https://doi.org/10.5155/eurjchem.7.1.19-29.1346
Design and synthesis of some new pyridopyrazinone derivatives as anti-proliferative agents is described. The cytotoxic activities of the synthesized compounds against melanoma...
2-(3-Bromophenyl)-8-fluoroquinazoline-4-carboxylic Acid as a Novel and Selective Aurora A Kinase Inhibitory Lead with Apoptosis Properties: Design, Synthesis, In Vitro and In Silico Biological Evaluation
Journal Article
Elsherbeny, M. H., Ammar, U. M., Abdellattif, M. H., Abourehab, M. A. S., Abdeen, A., Ibrahim, S. F., …Elkamhawy, A. (2022)
2-(3-Bromophenyl)-8-fluoroquinazoline-4-carboxylic Acid as a Novel and Selective Aurora A Kinase Inhibitory Lead with Apoptosis Properties: Design, Synthesis, In Vitro and In Silico Biological Evaluation. Life, 12(6), Article 876. https://doi.org/10.3390/life12060876
New quinazoline derivatives were designed based on the structural modification of the reported inhibitors to enhance their selectivity toward Aurora A. The synthesized compoun...