All Outputs (5)

Design, synthesis and anti-inflammatory activity of imidazol-5-yl pyridine derivatives as p38α/MAPK14 inhibitor (2020)
Journal Article
Ali, E. M., Abdel-Maksoud, M. S., Hassan, R. M., Mersal, K. I., Ammar, U. M., Se-In, C., He-Soo, H., Kim, H., Lee, A., Lee, K., & 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 inflammatory proteins (iNOS, NF-kB, and COX-2). In this study, drug repurposi... Read More about Design, synthesis and anti-inflammatory activity of imidazol-5-yl pyridine derivatives as p38α/MAPK14 inhibitor.

Design, synthesis, and biological evaluation of novel imidazole derivatives possessing terminal sulphonamides as potential BRAFV600E inhibitors (2020)
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 types. In the current work, a series of 38 4-(1H-imidazol-5-yl)pyridin-2-a... Read More about Design, synthesis, and biological evaluation of novel imidazole derivatives possessing terminal sulphonamides as potential BRAFV600E inhibitors.

Modification of imidazothiazole derivatives gives promising activity in B-Raf kinase enzyme inhibition; synthesis, in vitro studies and molecular docking (2020)
Journal Article
Ammar, U. M., Abdel-Maksoud, M. S., Mersal, K. I., Ali, E. M., Yoo, K. H., Choi, H. S., Lee, J. K., Cha, S. Y., & Oh, C. (2020). Modification of imidazothiazole derivatives gives promising activity in B-Raf kinase enzyme inhibition; synthesis, in vitro studies and molecular docking. Bioorganic and Medicinal Chemistry Letters, 30(20), Article 127478. https://doi.org/10.1016/j.bmcl.2020.127478

B-Raf mutation was identified as a key target in cancer treatment. Based on structural features of dabrafenib (potent FDA approved B-Raf inhibitor), the design of new NH2-based imidazothiazole derivatives was carried out affording new highly potent d... Read More about Modification of imidazothiazole derivatives gives promising activity in B-Raf kinase enzyme inhibition; synthesis, in vitro studies and molecular docking.

Structural optimization of imidazothiazole derivatives affords a new promising series as B-Raf V600E inhibitors; synthesis, in vitro assay and in silico screening (2020)
Journal Article
Ammar, U. M., Abdel-Maksoud, M. S., Ali, E. M., Mersal, K. I., Ho Yoo, K., & Oh, C. (2020). Structural optimization of imidazothiazole derivatives affords a new promising series as B-Raf V600E inhibitors; synthesis, in vitro assay and in silico screening. Bioorganic Chemistry, 100, Article 103967. https://doi.org/10.1016/j.bioorg.2020.103967

BRAF mutation is commonly known in a number of human cancer types. It is counted as a potential component in treating cancer. In this study, based on structural optimization of previously reported inhibitors (3-fluro substituted derivatives of imidaz... Read More about Structural optimization of imidazothiazole derivatives affords a new promising series as B-Raf V600E inhibitors; synthesis, in vitro assay and in silico screening.

Design and synthesis of novel pyrrolo[2,3-b]pyridine derivatives targeting V600EBRAF (2020)
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 approved V600E B-RAF inhibitors, two series of pyrrolo[2,3-b]pyridine scaffold... Read More about Design and synthesis of novel pyrrolo[2,3-b]pyridine derivatives targeting V600EBRAF.