A5001007309- Synthesis and biological activity
- Quinazolinone synthesis and applications
- HER2/EGFR in Cancer Research
- Cancer therapeutics and mechanisms
- Plant Disease Resistance and Genetics
- Lung Cancer Treatments and Mutations
- Click Chemistry and Applications
- Plant Disease Management Techniques
- Computational Drug Discovery Methods
- Synthesis and Characterization of Heterocyclic Compounds
- Chemotherapy-induced organ toxicity mitigation
- Antimicrobial Peptides and Activities
- Angiogenesis and VEGF in Cancer
- Free Radicals and Antioxidants
- PI3K/AKT/mTOR signaling in cancer
- Cell death mechanisms and regulation
- Multicomponent Synthesis of Heterocycles
- Bacterial biofilms and quorum sensing
- Synthesis of Tetrazole Derivatives
- Toxin Mechanisms and Immunotoxins
- Inflammatory mediators and NSAID effects
- Synthesis and Biological Evaluation
- Antimicrobial Resistance in Staphylococcus
- Nigella sativa pharmacological applications
- Bioactive Compounds and Antitumor Agents
Taibah University
2023-2025
Pharmac
2025
MCPHS University
2018
New phenyldiazene scaffold-linked heterocyclic pyrazole, pyrimidinone, pyrimidinthione, and/or triazine rings have been developed and synthesized. Cytotoxicity of our derivatives was estimated on four cancer VERO normal cell lines targeting EGFRT790M (epidermal growth factor receptor) VEGFR-2 (vascular endothelial receptor-2) enzymes. Our new selectively inhibited both EGFR as they the essential structural requirements for inhibitors receptors. Derivative 14 most active A549, HCT116, HepG2,...
A new series of thiazolyl-pyrazoline derivatives (4a–d, 5a–d 6a, b, 7a–d, 8a, and 10a, b) have been designed synthesized through the combination thiazole pyrazoline moieties, starting from key building blocks carbothioamides (1a–b). These eighteen as anticipated EGFR/HER2 dual inhibitors. The efficacy developed compounds in inhibiting cell proliferation was assessed using breast cancer MCF-7 line. Among thiazolyl-pyrazolines, 6b, 10b displayed potent anticancer activity toward with IC50 =...
Fifteen new iodoquinazoline derivatives, 5a,b to 18, are reported in this study and their anticancer evaluation as dual inhibitors of EGFR WT T790M .
The discovery of novel, selective inhibitors targeting CDK2 and PIM1 kinases, which regulate cell survival, proliferation, treatment resistance, is crucial for advancing cancer therapy. This study reports the design, synthesis, biological evaluation three novel pyrazolo[3,4-b]pyridine derivatives (6a-c), confirmed via spectral analyses. These compounds were assessed anti-cancer activity against breast, colon, liver, cervical cancers using MTT assay. Among tested compounds, 6b exhibited...
Pyrazole derivatives 2 and 3, pyrimidine derivative 4, their nanogels as drug delivery systems were synthesized, cytotoxicity against MCF-7, HCT-116, HepG2 A549 cells was evaluated.
Oxidative stress plays a significant role in the development of cancer. Inhibiting protein-protein interaction (PPI) between Keap1 and Nrf2 offers promising strategy to activate antioxidant pathway, which is normally suppressed by binding Nrf2. This study aimed identify natural compounds capable targeting kelch domain KEAP1 using structure-based drug design methods. A pharmacophore model was constructed based on KEAP1-inhibitor complex, leading selection 6178 that matched model....
Fifteen new 1-alkyl-6-iodoquinazoline derivatives 5a–d to 9a–e were designed and synthesized their anticancer activities evaluated against HepG2, MCF-7, HCT116 A549 cancer cell lines via dual targeting of EGFR VEGFR-2.
AbstractMicrobiological DNA gyrase is recognized as an exceptional microbial target for the innovative development of low-resistant and more effective antimicrobial drugs. Hence, we introduced a one-pot facile synthesis novel pyranopyrazole scaffold bearing different functionalities; substituted aryl ring, nitrile, hydroxyl groups. All new analogs were characterized with full spectroscopic data. The screening all was assessed against standard strains Gm + ve Gm-ve through in vitro considers....
Apoptosis is a critical process that regulates cell survival and death plays an essential role in cancer development. The Bcl-2 protein family, including myeloid leukemia 1 (Mcl-1), key regulator of the intrinsic apoptosis pathway, its overexpression many human cancers has prompted efforts to develop Mcl-1 inhibitors as potential anticancer agents. In this study, we aimed design new using various computational techniques. First, used receptor-ligand complex build e-pharmacophore hypothesis...
Novel inhibitors of epidermal growth factor receptor (EGFR)
Phenylpyrazolo[3,4-d]pyrimidine is considered a milestone scaffold known to possess various biological activities such as antiparasitic, antifungal, antimicrobial, and antiproliferative activities. In addition, the urgent need for selective potent novel anticancer agents represents major route in drug discovery process. Herein, new aryl analogs were synthesized evaluated their effects on panel of cancer cell lines: MCF-7, HCT116, HePG-2. Some these compounds showed cytotoxicity, with...
Antimicrobial resistance in methicillin-resistant Staphylococcus aureus (MRSA) is a major global health challenge.
A series of pyrazolopyrimidines derivatives 4– 11 were synthesized using 1-(6-(3-methoxyphenyl)-4-methylpyridazin-3-yl)-1H-pyrazolo [3,4-d] pyrimidin-4-amine 3 as a starting material. The detailed synthesis, structure assignments the novel compounds based on chemical and spectroscopic evidence, data, pharmacological properties molecular docking are reported. evaluation illustrated that many these have good analgesic, anti-inflammatory antimicrobial activities.
Black seed is often used as a spice in food and preservative many products. The main active constituent of black oil thymoquinone (TQ) which constitutes 30–57% the oil. Thymoquinone has shown varying therapeutic benefits various disease states, including cancer. aim this study was to investigate cytotoxic chemo‐sensitizing potential TQ compare it ethacrynic acid (EA), known agent sensitizing melanoma cells effects N‐mustards, chlorambucil (CHL) cyclophosphamide (CP). Both EA have an α, β...