A5050665287- Synthesis and biological activity
- Enzyme function and inhibition
- Synthesis and Catalytic Reactions
- Cancer therapeutics and mechanisms
- Cancer Mechanisms and Therapy
- Quinazolinone synthesis and applications
- Cholinesterase and Neurodegenerative Diseases
- Cytokine Signaling Pathways and Interactions
- Synthesis and Biological Evaluation
- Computational Drug Discovery Methods
- Click Chemistry and Applications
- X-ray Diffraction in Crystallography
- Synthesis and Characterization of Heterocyclic Compounds
- Crystallization and Solubility Studies
- Biochemical and Molecular Research
- Ubiquitin and proteasome pathways
- Microtubule and mitosis dynamics
- Cancer Research and Treatments
- Phenothiazines and Benzothiazines Synthesis and Activities
- Synthesis of heterocyclic compounds
- Protein Kinase Regulation and GTPase Signaling
- Coagulation, Bradykinin, Polyphosphates, and Angioedema
- COVID-19 Clinical Research Studies
- Phytochemical compounds biological activities
- Long-Term Effects of COVID-19
Tanta University
2019-2025
As a progressive neuropathic condition, glaucoma can cause lifelong blindness if left untreated. Novel phenylpyridazine-tethered sulfonamides were designed as selective inhibitors for carbonic anhydrase (CA) isoform II to find effective therapeutic agents glaucoma. Subsequently, the target synthesized and assessed their inhibitory action against cytosolic CA I II. Interestingly, molecules poorly inhibited while exhibiting low subnanomolar potency Compound
Telomerase is an outstanding biological target for cancer treatment. BIBR1532 a non-nucleoside selective telomerase inhibitor; however, it experiences ineligible pharmacokinetics. Herein, we aimed to design new BIBR1532-based analogues as promising inhibitors. Therefore, two novel series of pyridazine-linked cyclopenta[b]thiophene (8a-f) and tetrahydro-1-benzothiophene (9a-f) were synthesized. A quantitative real-time polymerase chain reaction was utilized investigate the inhibitory activity...
In this work, new isatin-based sulphonamides (6a-i, 11a-c, 12a-c) were designed and synthesised as potential dual VEGFR-2 carbonic anhydrase inhibitors with anticancer activities. Firstly, all target isatins examined for in vitro antitumor action on NCI-USA panel (58 tumour cell lines). Then, the most potent derivatives CA inhibitory towards physiologically relevant hCA isoforms I, II, tumour-linked IX isoform, addition, activity was evaluated. The failed to inhibit that could be...
A dual-targeting approach is predicted to yield better cancer therapy outcomes. Consequently, a series of coumarin-based thiazoles (5a–h, 6, and 7a–e) were designed constructed as potential carbonic anhydrase (CA) VEGFR-2 suppressors. The inhibitory actions the target compounds assessed against CA isoforms IX VEGFR-2. assay results showed that 5a, 5d, 5e can effectively inhibit both targets. cytotoxic effects tested on pancreatic, breast, prostate cells (PANC1, MCF7, PC3). Further...
With a "less is more" philosophy, series of 15 chalcone-sulfonamide hybrids were designed anticipating synergistic anticancer activity. The aromatic sulfonamide moiety was included as known direct inhibitor carbonic anhydrase IX activity through its zinc chelating property. chalcone incorporated an electrophilic stressor to indirectly inhibit cellular Screening by the Developmental Therapeutics Program National Cancer Institute, NCI-60, revealed that 12 derivatives potent inhibitors cancer...
Topoisomerase II (TOP-2) is a promising molecular target for cancer therapy. Numerous antibiotics could interact with biologically relevant macromolecules and provoke antitumor potential. Herein, docking studies were used to investigate the binding interactions of 138 against human topoisomerase II-DNA complex. Followed by MD simulations 200 ns MM-GBSA calculations. On other hand, activities most candidates investigated three cell lines using doxorubicin (DOX) as reference drug. Notably,...
Herein, modifications to the previously reported BIBR1591 were conducted obtain bioisosteric candidates with improved activities. The % inhibition of newly afforded against telomerase target was investigated. Notably, 6f achieved superior (63.14%) compared BIBR1532 and (69.64 51.58%, respectively). In addition, 8a 8b showed comparable promising 58.65 55.57%, respectively, which recorded be frontier that BIBR1591. 6f, 8a, tested five cancer cell lines related lung liver subtypes. Moreover,...
Donepezil-based rational design of N -substituted quinazoline tethered thioacetamide as potential acetylcholine esterase inhibitors for the treatment Alzheimer's disease.
Abstract New s ‐triazine hydrazone hybrids ( 4a – 4r ) were designed and synthesized as promising microbial DNA gyrase inhibitors. This was done by taking the lead inhibitor (AstraZeneca arylaminotriazine) a reference. The novel samples subsequently tested antimicrobial agents against certain pathogenic bacteria unicellular fungi. antibiofilm potential membrane leakage test used to determine mechanism of response. minimum inhibitory concentration (MIC) values 4g , 4i between 62.5 250.0...
Carbonic anhydrases (CAs) are one of the promising targets for development anticancer agents. CA isoforms implicated in various physiological processes and expressed both normal cancerous cells. Thus, non-isoform selective inhibitors associated with several side effects. Consequently, designing towards cancer-related hCA IX/XII rather than ubiquitous cytosolic isozymes I II is main research objective field. Herein, a new series 3-(6-methylpyridin-2-yl)coumarin derivatives 3 5a-o was designed...
Telomeres serve a critical function in cell replication and proliferation at every stage of the cycle. Telomerase is ribonucleoprotein, responsible for maintaining telomere length chromosomal integrity frequently dividing cells. Although it silenced most human somatic cells, restoration occurs cancer cells because telomerase activation or alternative lengthening. The enzyme universal anticancer target that expressed 85-95% cancers. BIBR1532 selective non-nucleoside potent inhibitor acts by...
Herein we reported the design and synthesis of two series comprising twenty-two benzenesulfonamides that integrate s-triazine moiety. Target compounds successfully suppressed hCA IX, with IC50 ranging from 28.6 to 871 nM. Compounds 5d, 11b, 5b, 7b were most active analogues, which inhibited IX isoform in low nanomolar range (KI = 28.6, 31.9, 33.4, 36.6 nM, respectively). Furthermore, they assessed for their cytotoxic activity against a panel 60 cancer cell lines following US-NCI protocol....