Outputs (4)

Scaffold Repurposing of In-House Small Molecule Candidates Leads to Discovery of First-in-Class CDK-1/HER-2 Dual Inhibitors: In Vitro and In Silico Screening (2021)
Journal Article
Elkamhawy, A., Ammar, U., Paik, S., Abdellattif, M. H., Elsherbeny, M. H., Lee, K., & Joo Roh, E. (2021). Scaffold Repurposing of In-House Small Molecule Candidates Leads to Discovery of First-in-Class CDK-1/HER-2 Dual Inhibitors: In Vitro and In Silico Screening. Molecules, 26(17), Article 5324. https://doi.org/10.3390/molecules26175324

Recently, multitargeted drugs are considered a potential approach in treating cancer. In this study, twelve in-house indole-based derivatives were preliminary evaluated for their inhibitory activities over VEGFR-2, CDK-1/cyclin B and HER-2. Compound... Read More about Scaffold Repurposing of In-House Small Molecule Candidates Leads to Discovery of First-in-Class CDK-1/HER-2 Dual Inhibitors: In Vitro and In Silico Screening.

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 (2021)
Journal Article
Mersal, K. I., Abdel-Maksoud, M. S., Ali, E. M. H., Ammar, U. M., Zaraei, S.-O., Kim, J.-M., Kim, S.-Y., Lee, K.-T., Lee, K. H., Kim, S.-W., Park, H.-M., Ji, M.-J., & Oh, C.-H. (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 cytotoxic effect of the final compounds was measured by applying MTT assay in... Read More about 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.

Discovery of New Imidazo[2,1-b]thiazole Derivatives as Potent Pan-RAF Inhibitors with Promising In Vitro and In Vivo Anti-melanoma Activity (2021)
Journal Article
Abdel-Maksoud, M. S., El-Gamal, M. I., Lee, B. S., Gamal El-Din, M. M., Jeon, H. R., Kwon, D., Ammar, U. M., Mersal, K. I., Ali, E. M. H., Lee, K.-T., Yoo, K. H., Han, D. K., Lee, J. K., Kim, G., Choi, H. S., Kwon, Y. J., Lee, K. H., & Oh, C. H. (2021). Discovery of New Imidazo[2,1-b]thiazole Derivatives as Potent Pan-RAF Inhibitors with Promising In Vitro and In Vivo Anti-melanoma Activity. Journal of Medicinal Chemistry, 64(10), 6877-6901. https://doi.org/10.1021/acs.jmedchem.1c00230

BRAF is an important component of MAPK cascade. Mutation of BRAF, in particular V600E, leads to hyperactivation of the MAPK pathway and uncontrolled cellular growth. Resistance to selective inhibitors of mutated BRAF is a major obstacle against treat... Read More about Discovery of New Imidazo[2,1-b]thiazole Derivatives as Potent Pan-RAF Inhibitors with Promising In Vitro and In Vivo Anti-melanoma Activity.

Design, synthesis, biological evaluation, and docking studies of novel (imidazol-5-yl)pyrimidine-based derivatives as dual BRAFV600E/p38α inhibitors (2021)
Journal Article
Ali, E. M., El-Telbany, R. F. A., Abdel-Maksoud, M. S., Ammar, U. M., Mersal, K. I., Zaraei, S.-O., El-Gamal, M. I., Choi, S.-I., Lee, K.-T., Kim, H.-K., Lee, K. H., & Oh, C.-H. (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 benefits for treatment of these diseases. In the present work, a new series o... Read More about Design, synthesis, biological evaluation, and docking studies of novel (imidazol-5-yl)pyrimidine-based derivatives as dual BRAFV600E/p38α inhibitors.