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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., Haque, M. M., …Oh, C. (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., …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., …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., Choi, H. S., Yoo, K. H., Han, D. K., Oh, C. H., Mohammed, A., …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., Abdel-Maksoud, M. S., El-Gamal, M. I., …Oh, C. (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.

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., 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 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., …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., …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 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.

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., …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., …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.

Design, synthesis, and anticancer activity of imidazo[2,1-b]oxazole-based RAF kinase inhibitors (2019)
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-RAF inhibitors. The twenty two final compounds were tested over A375 and SKM... Read More about Design, synthesis, and anticancer activity of imidazo[2,1-b]oxazole-based RAF kinase inhibitors.

Synthesis and In Vitro Biological Evaluation of New Pyrido[2,3‐b]pyrazinone‐Based Cytotoxic Agents and Molecular Docking as BRAF Inhibitors (2019)
Journal Article
Amin, K., El‐Badry, O., Abdel Rahman, D., & Ammar, U. (2019). Synthesis and In Vitro Biological Evaluation of New Pyrido[2,3‐b]pyrazinone‐Based Cytotoxic Agents and Molecular Docking as BRAF Inhibitors. ChemistrySelect, 4(30), 8882-8885. https://doi.org/10.1002/slct.201901487

In this study, synthesis of new pyrido[2,3-b]pyrazinone derivatives were identified. The in vitro cytotoxic activity of synthesized compounds against human colon cancer cell line (HCT 116) and kinase assay (V600EBRAF) were investigated. The results r... Read More about Synthesis and In Vitro Biological Evaluation of New Pyrido[2,3‐b]pyrazinone‐Based Cytotoxic Agents and Molecular Docking as BRAF Inhibitors.

Anticancer profile of newly synthesized BRAF inhibitors possess 5-(pyrimidin-4-yl)imidazo[2,1-b]thiazole scaffold (2019)
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 pyrimidine ring at position 5. The pyrimidine ring containing either amide or s... Read More about Anticancer profile of newly synthesized BRAF inhibitors possess 5-(pyrimidin-4-yl)imidazo[2,1-b]thiazole scaffold.

Recent advances of RAF (rapidly accelerated fibrosarcoma) inhibitors as anti-cancer agents (2018)
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 cancer initiation, in particular RAF (rapidly accelerated fibrosarcoma) comp... Read More about Recent advances of RAF (rapidly accelerated fibrosarcoma) inhibitors as anti-cancer agents.

Design, synthesis, anticancer evaluation and molecular docking of new V600EBRAF inhibitors derived from pyridopyrazinone (2016)
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 cell line (LOXIMVI), ovarian cell line (OVCAR3), thyroid cell lines (CAL62... Read More about Design, synthesis, anticancer evaluation and molecular docking of new V600EBRAF inhibitors derived from pyridopyrazinone.