Outputs (23)

Discovery of Benzopyrone-Based Candidates as Potential Antimicrobial and Photochemotherapeutic Agents through Inhibition of DNA Gyrase Enzyme B: Design, Synthesis, In Vitro and In Silico Evaluation (2024)
Journal Article
Abd El-Haleem, A., Ammar, U., Masci, D., El-Ansary, S., Abdel Rahman, D., Abou-Elazm, F., & El-Dydamony, N. (2024). Discovery of Benzopyrone-Based Candidates as Potential Antimicrobial and Photochemotherapeutic Agents through Inhibition of DNA Gyrase Enzyme B: Design, Synthesis, In Vitro and In Silico Evaluation. Pharmaceuticals, 17(9), Article 1197. https://doi.org/10.3390/ph17091197

Bacterial DNA gyrase is considered one of the validated targets for antibacterial drug discovery. Benzopyrones have been reported as promising derivatives that inhibit bacterial DNA gyrase B through competitive binding into the ATP binding site of th... Read More about Discovery of Benzopyrone-Based Candidates as Potential Antimicrobial and Photochemotherapeutic Agents through Inhibition of DNA Gyrase Enzyme B: Design, Synthesis, In Vitro and In Silico Evaluation.

Design and Synthesis of Novel Aminoindazole-pyrrolo[2,3-b]pyridine Inhibitors of IKKα That Selectively Perturb Cellular Non-Canonical NF-κB Signalling (2024)
Journal Article
Riley, C., Ammar, U., Alsfouk, A., Anthony, N. G., Baiget, J., Berretta, G., Breen, D., Huggan, J., Lawson, C., McIntosh, K., Plevin, R., Suckling, C. J., Young, L. C., Paul, A., & Mackay, S. P. (2024). Design and Synthesis of Novel Aminoindazole-pyrrolo[2,3-b]pyridine Inhibitors of IKKα That Selectively Perturb Cellular Non-Canonical NF-κB Signalling. Molecules, 29(15), Article 3515. https://doi.org/10.3390/molecules29153515

The inhibitory-kappaB kinases (IKKs) IKKα and IKKβ play central roles in regulating the non-canonical and canonical NF-κB signalling pathways. Whilst the proteins that transduce the signals of each pathway have been extensively characterised, the cle... Read More about Design and Synthesis of Novel Aminoindazole-pyrrolo[2,3-b]pyridine Inhibitors of IKKα That Selectively Perturb Cellular Non-Canonical NF-κB Signalling.

Correction: Elsherbeny et al. 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 2022, 12, 876 (2024)
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. (2024). Correction: Elsherbeny et al. 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 2022, 12, 876. Life, 14(4), 423. https://doi.org/10.3390/life14040423

In the original publication [1], reference number 26 [2] was added by mistake. Thus, it was removed.

With this correction, the order of some references has been adjusted accordingly. The authors state that the scientific conclusions are unaffected... Read More about Correction: Elsherbeny et al. 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 2022, 12, 876.

Abstract 4472: Discovery of potential RAF-selective back pocket as a promising biological target for BRAF inhibitors in the treatment of resistant melanoma: Design, synthesis, biological evaluation and in silico studies (2024)
Presentation / Conference Contribution
Ammar, U., Gamal, M., Abdel-Maksoud, M., Ali, E., Mahmoud, Z., Deug, K., Jun, P., Lee, S., & Oh, C. Abstract 4472: Discovery of potential RAF-selective back pocket as a promising biological target for BRAF inhibitors in the treatment of resistant melanoma: Design, synthesis, biological evaluation and in silico studies. Presented at American Association for Cancer Research Annual Meeting 2024, San Diego, CA

The mutated BRAF kinase (V600E) is considered the key component in the MAPK signaling pathway that was reported to be significantly contributed to melanoma disease. Vemurafenib and dabrafenib are examples of drugs that were approved by FDA to treat m... Read More about Abstract 4472: Discovery of potential RAF-selective back pocket as a promising biological target for BRAF inhibitors in the treatment of resistant melanoma: Design, synthesis, biological evaluation and in silico studies.

Evaluation of novel pyrazol-4-yl pyridine derivatives possessing arylsulfonamide tethers as c-Jun N-terminal kinase (JNK) inhibitors in leukemia cells (2023)
Journal Article
Mersal, K. I., Abdel-Maksoud, M. S., Ali, E. M., Ammar, U. M., Zaraei, S.-O., Haque, M. M., Das, T., Hassan, N. F., Kim, E. E., Lee, J.-S., Park, H., Lee, K. H., El-Gamal, M. I., Kim, H.-K., Ibrahim, T. M., & Oh, C.-H. (2023). Evaluation of novel pyrazol-4-yl pyridine derivatives possessing arylsulfonamide tethers as c-Jun N-terminal kinase (JNK) inhibitors in leukemia cells. European Journal of Medicinal Chemistry, 261, Article 115779. https://doi.org/10.1016/j.ejmech.2023.115779

A series of 36 pyrazol-4-yl pyridine derivatives (8a-i, 9a-i, 10a-i, and 11a-i) was designed, synthesized, and evaluated for its antiproliferative activity over NCI-60 cancer cell line panel and inhibitory effect against JNK isoforms (JNK1, JNK2, and... Read More about Evaluation of novel pyrazol-4-yl pyridine derivatives possessing arylsulfonamide tethers as c-Jun N-terminal kinase (JNK) inhibitors in leukemia cells.

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.

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.