Outputs (4)

Scaffold Repurposing Reveals New Nanomolar Phosphodiesterase Type 5 (PDE5) Inhibitors Based on Pyridopyrazinone Scaffold: Investigation of In Vitro and In Silico Properties (2022)
Journal Article
Amin, K. M., El-Badry, O. M., Abdel Rahman, D. E., Abdellattif, M. H., Abourehab, M. A. S., El-Maghrabey, M. H., Elsaid, F. G., El Hamd, M. A., Elkamhawy, A., & Ammar, U. M. (2022). Scaffold Repurposing Reveals New Nanomolar Phosphodiesterase Type 5 (PDE5) Inhibitors Based on Pyridopyrazinone Scaffold: Investigation of In Vitro and In Silico Properties. Pharmaceutics, 14(9), Article 1954. https://doi.org/10.3390/pharmaceutics14091954

Inhibition of PDE5 results in elevation of cGMP leading to vascular relaxation and reduction in the systemic blood pressure. Therefore, PDE5 inhibitors are used as antihypertensive and antianginal agents in addition to their major use as male erectil... Read More about Scaffold Repurposing Reveals New Nanomolar Phosphodiesterase Type 5 (PDE5) Inhibitors Based on Pyridopyrazinone Scaffold: Investigation of In Vitro and In Silico Properties.

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 (2022)
Journal Article
Elsherbeny, M. H., Ammar, U. M., Abdellattif, M. H., Abourehab, M. A. S., Abdeen, A., Ibrahim, S. F., Abdelrahaman, D., Mady, W., Roh, E. J., & 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 compounds were tested over Aurora A, and a cytotoxicity assay was performed over N... Read More about 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.

Imidazooxazole derivative having antitumor effect, and pharmaceutical compostion including same (2022)
Patent
Mahmoud, G. E.-D., Choi, H. S., Yoo, K. H., Han, D. K., Oh, C. H., Mohammed, A.-M., Mohammed, I. E.-G., & Ammar, U. (2022). Imidazooxazole derivative having antitumor effect, and pharmaceutical compostion including same. US011332479B2

Provided is a pharmaceutical composition for preventing and treating tumors, the pharmaceutical composition including an imidazooxazole derivative compound, a solvate, a stereoisomer, or a pharmaceutically acceptable salt thereof as an active ingredi... Read More about Imidazooxazole derivative having antitumor effect, and pharmaceutical compostion including same.

Structural optimization of 4-(imidazol-5-yl)pyridine derivatives affords broad-spectrum anticancer agents with selective B-RAFV600E/p38α kinase inhibitory activity: Synthesis, in vitro assays and in silico study (2022)
Journal Article
Ali, E. M., Mersal, K. I., Ammar, U. M., Zaraei, S.-O., Abdel-Maksoud, M. S., El-Gamal, M. I., Haque, M. M., Das, T., Kim, E. E., Lee, J.-S., Lee, K. H., Kim, H.-K., & Oh, C.-H. (2022). Structural optimization of 4-(imidazol-5-yl)pyridine derivatives affords broad-spectrum anticancer agents with selective B-RAFV600E/p38α kinase inhibitory activity: Synthesis, in vitro assays and in silico study. European Journal of Pharmaceutical Sciences, 171, Article 106115. https://doi.org/10.1016/j.ejps.2022.106115

In the current article, we introduce design of a new series of 4-(imidazol-5-yl)pyridines with improved anticancer activity and selective B-RAF V600E /p38α kinase inhibitory activity. Based on a previous work, a group of structural modifications were... Read More about Structural optimization of 4-(imidazol-5-yl)pyridine derivatives affords broad-spectrum anticancer agents with selective B-RAFV600E/p38α kinase inhibitory activity: Synthesis, in vitro assays and in silico study.