A5103259332- Synthesis and biological activity
- Synthesis and Characterization of Heterocyclic Compounds
- Computational Drug Discovery Methods
- Cancer therapeutics and mechanisms
- Bioactive Compounds and Antitumor Agents
- Cholinesterase and Neurodegenerative Diseases
- Click Chemistry and Applications
- Cell death mechanisms and regulation
- Genomics, phytochemicals, and oxidative stress
- Synthesis and Biological Evaluation
- Redox biology and oxidative stress
- Protein Tyrosine Phosphatases
- Hormonal and reproductive studies
- Biochemical and Molecular Research
- Cancer Mechanisms and Therapy
- Synthesis and Reactions of Organic Compounds
- Enzyme function and inhibition
- Pharmacogenetics and Drug Metabolism
- Free Radicals and Antioxidants
- Quinazolinone synthesis and applications
- Plant-Derived Bioactive Compounds
- Signaling Pathways in Disease
- Glutathione Transferases and Polymorphisms
- Cancer-related Molecular Pathways
- Prostate Cancer Treatment and Research
Ankara University
2013-2023
Background: Pyrrolo[2,3-d]pyrimidines have been recently reported to anticancer activities through inhibition of different targets such as, Epidermal Growth Factor Receptor (EGFR) tyrosine kinase, Janus Kinase (JAK), mitotic checkpoint protein kinase (Mps1), carbonic anhydrase, MDM-2. On the other hand, aryl urea moieties which are found in some inhibitors as Sorafenib and Linifanib aroused recent attention responsible for activities. The aims this paper synthesize pyrrolo[ 2,3-d]pyrimidine...
Several substituted indolin-2-one derivatives were synthesized and evaluated for their activities against Src kinase. compounds showed activity Src, with IC50 values in the low micromolar range. Among them, compound 2f most significant an value of 1.02 μM. Molecular docking studies have been performed evaluation binding modes into active site. The structure disclosed that indole NH forms a hydrogen bond carbonyl Met341. These results suggest our novel is promising further development...
<i>Background:</i> Oxidative stress has been implicated in aging and a variety of diseases affecting the nervous, respiratory, cardiovascular gastrointestinal system humans. Reactive oxygen species (ROS) have associated with mechanisms to activate kinases, such as protein tyrosine which may initiate malignant transformation. Significant evidences activation kinases by oxidative brought increased attention role antioxidants these mechanisms. Therefore, recent efforts focused on...
In this work, a series of piperazine substituted indole derivatives were synthesized and evaluated for their in vitro antioxidant anti-inflammatory activities.The results activity showed that compounds 2 (81.63%) 11 (85.63%) had comparable DPPH free radical scavenging to Vit E (88.6%).The antiinflammatory assays indicated most the more higher activities than standart ASA.Docking revealed compound possessing strongest Hbond interactions with key residues COX-2 active site.It suggested might...
Abstract A series of novel indole hydrazide derivatives was synthesized and evaluated for their anticancer activities. Compound 12 exhibited the highest antiproliferative activity against MCF‐7 cell line, with an IC 50 value 3.01 µM. Treatment cells compound led to cycle arrest at G0/G1 phase also displayed a significant annexin V binding pattern, indicating that is effective in apoptotic death. The Western blot analysis showed increased expression proapoptotic Bax decreased levels...
In this work, synthesis of novel 1,3,4-oxadiazole derivatives were reported. Good molecular properties profile was predicted for the target compounds. drug likeness prediction, compound 4b and 8b possess highest score 0.31 0.33, respectively. Since compounds have good bioactivity scores as kinase inhibitor, possible interactions with VEGFR-2 probable binding conformations evaluated by docking. All formed hydrogen bonding Asp1046 amino acid key residues.
Matrix metalloproteinases are known as extracellular matrix degrading enzymes and have important role on tumor progression.This study reports the effects of 1,3,5-trisubstituted indole derivatives cytotoxicity, apoptosis MMP- 2/MMP-9 mRNA expression MCF-7 human breast carcinoma cells.The cytotoxic compounds cells were performed by MTT test, cell proliferation was determined via BrdU incorporation. The apoptotic observed death detection elisa. MMP-2/-9 enzyme activity also performed.The...
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In this present work, 5-chloro-3-(substituted-benzylidene)indolin-2-one and 1-benzyl-5-chloro-3-(substitutedbenzylidene) indolin-2-one derivatives were synthesized evaluated for their inhibitory activity against Src Family Kinases (SFKs) such as Fyn, Lyn Hck. 5-Chloro-3-(substituted)indolin-2-ones (3a - 6a) 1-benzyl-5-chloro-3- (substituted-benzylidene)indolin-2-ones (3b 6b) prepared by condensation of 5-chloro oxindole 1-benzyl-5- chloro with the equivalent amount aldehydes in EtOH presence...
The aim of this study is to design and synthesize novel dual inhibitors Src protein tyrosine kinase (PTK) Glutathione S-transferases (GSTs), as a potential drug lead with therapeutic efficacy on cancer immune disorders. biological activity profiling small molecule via miniaturized biochemical techniques compatible medium throughput screening focused methodologies were performed. To determining the effects Phase II detoxification enzyme GST isozymes in liver homogenates used verify their...
With the aim to overcome lack of potent and selective Hyaluronidases (Hyals) inhibitors, we have tested new 1, 3 5 substituted indole derivatives for inhibition bovine testicular hyaluronidases (BTH) in a stains-all assay at pH 7 Morgan-Elson 3.5. Most compounds are found as activator Although amine 17 18 did not show BTH 7, they reacted most activators On other hand, some imine inhibitors compound 25 was inhibitor. Keywords: Hyaluronidase, Indole derivatives, Inhibition, assay, Stains all...