A5008179990- Synthesis and biological activity
- Free Radicals and Antioxidants
- Click Chemistry and Applications
- Retinoids in leukemia and cellular processes
- Computational Drug Discovery Methods
- Synthesis and Characterization of Heterocyclic Compounds
- Circadian rhythm and melatonin
- Synthesis and Biological Evaluation
- Neuroscience and Neuropharmacology Research
- Antioxidant Activity and Oxidative Stress
- Pharmacological Receptor Mechanisms and Effects
- Phenothiazines and Benzothiazines Synthesis and Activities
- Bioactive Compounds and Antitumor Agents
- Prostate Cancer Treatment and Research
- Cancer therapeutics and mechanisms
- Estrogen and related hormone effects
- Synthesis of Organic Compounds
- Synthesis of heterocyclic compounds
- Quinazolinone synthesis and applications
- HIV/AIDS drug development and treatment
- Metal complexes synthesis and properties
- Receptor Mechanisms and Signaling
- Crystallization and Solubility Studies
- Cell death mechanisms and regulation
- X-ray Diffraction in Crystallography
Ankara University
2010-2024
University of the Sciences
2011-2020
A series of alkylsulfonyl 1H-benzo[d]imidazole derivatives were synthesized and evaluated for anticancer activity against human breast cancer cells, MCF-7 in vitro. The cytotoxic potential was determined using the xCELLigence real-time cell analysis, expression levels genes related to microtubule organization, tumor suppression, apoptosis, cycle, proliferation examined by quantitative polymerase chain reaction. Molecular docking Bcl-2 carried out AutoDock Vina, while ADME studies performed...
As part of our program to explore the influence small structural modifications drug candidate 3β-(hydroxy)-17-(1H-benzimidazol-1-yl)androsta-5,16-diene (galeterone, 5) on modulation androgen receptor (AR), we have prepared and evaluated a series novel C-3, C-16, C-17 analogues. Using structure activity analysis, established that benzimidazole moiety at is essential optimal also hydrophilic heteroaromatic groups C-3 enhance both antiproliferative (AP) AR degrading (ARD) activities. The most...
Depression is a psychiatric disorder that affects millions of people worldwide. Individuals battling this commonly experience high rates relapse, persistent residual symptoms, functional impairment, and diminished well-being. Medications have important utility in stabilizing moods daily functions many individuals. However, only one third patients had considerable improvement with standard antidepressant after 2 months all to deal numerous side effects. The N-methyl-d-aspartate (NMDA)...
Some 6-fluoro-5-substituted-benzimidazole derivatives in which indole and 1,1,4,4-tetramethyl-1,2,3,4-tetrahydro-naphthalene groups were attached to the 2-position of benzimidazole ring synthesized tested for antioxidant properties vitro. Almost all compounds at 10(-3) M concentrations showed superoxide anion scavenging activity. Compounds 5, 3, 9, 4, 17 13 have strong inhibitory effects on formation (98%, 93%, 91%, 88%, 85% 81%, respectively) concentration these results are better than 30...
Novel retinoid derivatives containing a benzimidazole moiety were synthesized and tested for their antimicrobial activity. Their activities against methicillin-resistant <i>Staphylococcus aureus </i>(MRSA), aureus</i>, <i>Escherichia coli, Pseudomonas aeruginosa, Enterococcus faecalis, Candida krusei</i> <i>Candida albicans</i> evaluated. While some of the compounds exhibited moderate activity MRSA, <i>S. aureus, E. C. krusei albicans,...
Phenothiazines (PTZ) are antipsychotics known to modulate a variety of neurotransmitter activities that include dopaminergic and cholinergic signaling have been identified as potential anticancer agents in vitro. However, it is important also test whether highly cytotoxic, repurposed, or novel PTZ has low toxicity neuromodulatory activity vivo using vertebrate model organisms, such zebrafish. In this study, we synthesized phenothiazines screened them vitro liver cancer zebrafish...
Specific sidechain modifications on the indole-benzimidazole scaffold play fundamental roles for determining molecule's affinity against ERα and its anti-cancer activity.
Abstract Our approach was to examine the antioxidant activity of novel retinoid derivatives containing benzimidazole moiety. Their in vitro effects on rat liver microasomal, NADPH‐dependent lipid peroxidation levels and superoxide anion formation were determined. Lipid microsomes reduced by some compounds a dose‐dependent manner.
Abstract magnified image A series of 47 novel N 1 ‐alkylated‐2‐aryl‐5(6)‐substituted‐1 H ‐benzimidazoles and their three indole analogues were synthesized evaluated for in vitro antifungal activities against Candida species by the tube dilution method. The results showed that compounds 79 80 , having pyridine at position C‐2, benzimidazoles exhibited greatest activity with MIC values 6.25–3.12 μg/mL. Indole 108‐110 have no inhibitory activity. J. Heterocyclic Chem., (2009).
Vanadium is a widely used transition metal in industrial applications, but it also poses significant neurotoxic and environmental risks. Previous studies have shown that exposure to vanadium may lead neurodegenerative diseases neuropathic pain, raising concerns about its impact on human health the ecosystem. To address neurotoxicity, through targeting NMDA glutamate dopamine signaling, both involved disorders, shows promise. Using Caenorhabditis elegans as model, we evaluated novel compound...
Retinoids, synthetic and natural analogues of a//-iram-retinoic acid (RA), exert their biological effects with responsive elements DNA to promote on cell differentiation proliferation behave as potent adipogenic hormones.Herein, we describe the synthesis a number novel tetrahydrotetramethylnaphthalene benzimidazole derivatives retinoids.Analogs were prepared depicted in Scheme 1 2. As is evident from both shemes.a variety have been synthesized by using an appropiate NaHS0 3 addiction product
Abstract Several 2‐(5,5,8,8‐tetramethyl‐5,6,7,8‐tetrahydronaphthalen‐2‐yl)‐1 H ‐benzimidazole‐5‐carboxamidine analogues were synthesized for their antibacterial and antifungal activities against S. aureus, Methicillin ‐ resistant aureus (MRSA) , C. albicans krusei . MIC values of the targeted compounds 43 58 are comparable to those Fluconazole Sultamicillin. The most potent compounds, 51 53 showed as 0.78 1.56 μg/mL respectively.
A number of retinoid-related compounds represent classes antioxidative and proapoptotic agents with promising potential in the treatment neoplastic diseases. Indeed, synthetic retinoid amide fenretinide [N-(4-hydroxyphenyl)retinamide] induces apoptosis cancer cells acts as a chemotherapeutic drug therapy. In present work, continuation our studies on retinoid-type compounds, synthesis melatonin retinamide derivatives was studied novel series retinoids, using condensation reaction sequence...
Several indole-thiazolidinedione derivatives ( 9–24 ) were designed and synthesized as CDK6 inhibitors, their anticancer activity was probed on the MCF-7 cell line effects gene expression profiles elucidated.
Abstract magnified image As part of an ongoing program aimed at recognizing novel antioxidant, antimicrobial, and anticancer molecules, herein we report the synthesis biological evaluation imidazolidin‐4‐one thiazolidine‐2,4‐dione derivatives as antimicrobial agents. These compounds were prepared from 5,5,8,8‐tetramethyl‐5,6,7,8‐tetrahydro‐naphthalen‐2‐carboxaldehyde 3‐substituted phenacyl‐2,4‐thiazolidinediones using Knoevenagel reaction. The structures confirmed by 1 H NMR, mass spectral...
Series of 4-(ethylsulfonyl)-1-halogen-2-nitrobenzene (3a-e) and 1-(4-halogen-3-nitrophenyl) propan-1-one (5a-d) analogs designed as novel radiosensitizers using bromonitropropiophenone bromonitrobenzonitrile lead compounds were synthesized. The anticancer activities the evaluated in vitro human prostate cancer (DU-145) breast (MCF-7) cell lines MTT assay. From series, six (3b-e, 5b-c) exhibited potent growth inhibitory effects against both lines. most active, compound 3d, is an iodosulfone...
Several novel norcamphor (bicycloheptane)-based compounds were designed and synthesized as non-competitive N-methyl-D-aspartate receptor antagonists at the phencyclidine binding sites. The heterocyclic ring was also varied to examine piperidine, pyrrolidine, morpholine groups. We examined pharmacological activities of these in vitro (binding studies) vivo (maximal electroshock test). Pharmacological evaluations revealed one compounds, 5a, be a good lead, exhibiting moderate receptors (IC(50)...