A5076621914- Melanoma and MAPK Pathways
- Synthesis and biological activity
- Computational Drug Discovery Methods
- Cytokine Signaling Pathways and Interactions
- Cancer Mechanisms and Therapy
- Cancer therapeutics and mechanisms
- Cancer-related Molecular Pathways
- Synthesis and Biological Evaluation
- Microtubule and mitosis dynamics
- Quinazolinone synthesis and applications
- Enzyme function and inhibition
- Synthesis of Tetrazole Derivatives
- Synthesis of heterocyclic compounds
- interferon and immune responses
- HER2/EGFR in Cancer Research
- Bioactive Compounds and Antitumor Agents
- Cholinesterase and Neurodegenerative Diseases
- Biochemical and Molecular Research
- 14-3-3 protein interactions
- Phosphodiesterase function and regulation
- NF-κB Signaling Pathways
Edinburgh Napier University
2023-2025
University of Strathclyde
2020-2024
Korea Institute of Science and Technology
2018-2020
Ahram Canadian University
2016-2020
Korea University of Science and Technology
2018-2020
Raf kinase enzymes are often dysregulated in melanoma. While sorafenib demonstrates strong activity against wild-type B-Raf, it fails to effectively inhibit the mutated form of B-Raf. In this study, served as a lead compound for development new derivatives designed enhance inhibitory across multiple isoforms (pan-Raf inhibitors). Novel naphthalene-based diarylamide were subsequently designed, synthesized, and evaluated their biological various melanoma A375 cell line. Among these, 9a,...
BRAF is an important component of MAPK cascade. Mutation BRAF, in particular V600E, leads to hyperactivation the pathway and uncontrolled cellular growth. Resistance selective inhibitors mutated a major obstacle against treatment many cancer types. In this work, series new (imidazo[2,1-b]thiazol-5-yl)pyrimidine derivatives possessing terminal sulfonamide moiety were synthesized. Pan-RAF inhibitory effect was investigated, structure–activity relationship discussed. Antiproliferative activity...
The inhibitory-kappaB kinases (IKKs) IKKα and IKKβ play central roles in regulating the non-canonical canonical NF-κB signalling pathways. Whilst proteins that transduce signals of each pathway have been extensively characterised, clear dissection functional IKKα-mediated versus IKKβ-driven remains to be fully elucidated. Progress has relied upon complementary molecular pharmacological tools; however, lack highly potent selective inhibitors limited advances. Herein, we report development an...
In the current article, we introduce design of a new series 4-(imidazol-5-yl)pyridines with improved anticancer activity and selective B-RAFV600E/p38α kinase inhibitory activity. Based on previous work, group structural modifications were applied affording potential antiproliferative agents. Towards extensive biological assessment target compounds, an in vitro assay was conducted over NCI 60-cancer cell lines panel representing blood, lung, colon, CNS, skin, ovary, renal, prostate, breast...
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 15l showed the most among tested was its selectivity small kinase panel. It dual Moreover, vitro cytotoxicity assay assessed selected series against nine NCI cell lines. potent compounds. A deep silico molecular docking study conducted compound...
Design and synthesis of some new pyridopyrazinone derivatives as anti-proliferative agents is described. The cytotoxic activities the synthesized compounds against melanoma cell line (LOXIMVI), ovarian (OVCAR3), thyroid lines (CAL62, FTC133, BCPAP ML1) colon (HT29 HCT116) were investigated. Results revealed that most active compound 3d was one. It exhibited promising activity all tested lines. In addition, in vitro kinase assay both WT BRAF V600E performed for compounds. Furthermore,...
New quinazoline derivatives were designed based on the structural modification of reported inhibitors to enhance their selectivity toward Aurora A. The synthesized compounds tested over A, and a cytotoxicity assay was performed NCI cell lines select best candidate for further evaluation. Compound
Inhibition of PDE5 results in elevation cGMP leading to vascular relaxation and reduction the systemic blood pressure. Therefore, inhibitors are used as antihypertensive antianginal agents addition their major use male erectile dysfunction treatments. Previously, we developed a novel series 34 pyridopyrazinone derivatives anticancer (series A-H). Herein, multi-step silico approach was preliminary conducted evaluate predicted inhibitory activity, followed by an vitro biological evaluation...
Abstract The mutated BRAF kinase (V600E) is considered the key component in MAPK signaling pathway that was reported to be significantly contributed melanoma disease. Vemurafenib and dabrafenib are examples of drugs were approved by FDA treat through inhibition (V600E). However, drug resistance after 6 - 7 months treatment using these due activation this another RAF (CRAF). As a Drug Discovery research group, we interested study identify possible biological target inhibit resistant form...
Bacterial DNA gyrase is considered one of the validated targets for antibacterial drug discovery. Benzopyrones have been reported as promising derivatives that inhibit bacterial B through competitive binding into ATP site subunit. In this study, we designed and synthesized twenty-two benzopyrone-based with different chemical features to assess their antimicrobial photosensitizing activities. The activity was evaluated against
Abstract In this study, synthesis of new pyrido[2,3‐ b ]pyrazinone derivatives were identified. The in vitro cytotoxic activity synthesized compounds against human colon cancer cell line (HCT 116) and kinase assay ( V600E BRAF) investigated. results revealed that 4 c (4‐nitro 4‐methoxy benzylidene acid hydrazide substitution, respectively) the most active among (IC 50 12.120 13.103 μM, respectively). Moreover, they exhibited inhibitory BRAF (Inh % 79.23 81.33, addition, designed subjected to...
A series of 36 pyrazol-4yl pyridine derivatives (8a-i, 9a-i, 10a-i, and 11a-i ) was designed, synthesized, evaluated for its antiproliferative activity over NCI-60 cancer cell line panel inhibitory effect against JNK isoforms (JNK1, JNK2, JNK3). All the synthesized compounds were tested panel. Compounds 11b, 11c, 11g, 11i selected to determine their GI50s exerted a superior potency than reference standard SP600125 lines. 11c showed GI50 1.28 μM K562 leukemic cells. Vero cells used assess...