A5067365083- Synthesis and biological activity
- Chemical synthesis and pharmacological studies
- Computational Drug Discovery Methods
- Crystallization and Solubility Studies
- Synthesis and Reactions of Organic Compounds
- X-ray Diffraction in Crystallography
- Synthesis and Biological Evaluation
- Synthesis and Characterization of Heterocyclic Compounds
- Free Radicals and Antioxidants
- Crystal structures of chemical compounds
- Crystallography and molecular interactions
- Synthesis of heterocyclic compounds
- Multicomponent Synthesis of Heterocycles
- Organic Chemistry Cycloaddition Reactions
- Click Chemistry and Applications
- Enzyme function and inhibition
- Phenothiazines and Benzothiazines Synthesis and Activities
- Bioactive Compounds and Antitumor Agents
- Synthesis and Reactivity of Heterocycles
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Structural and Chemical Analysis of Organic and Inorganic Compounds
- Organic Chemistry Synthesis Methods
- Peptidase Inhibition and Analysis
- HIV/AIDS drug development and treatment
- Biochemical and Molecular Research
Erciyes University
2014-2024
Bozok Universitesi
2008
Atatürk University
2005
University of Graz
1989-1990
Abstract (A new 4‐oxothiazolidin‐2‐ylidene derivative bearing hydrazone moiety was synthesized via Michael addition between the reaction of 4‐(4‐nitrophenyl)‐3‐thiosemicarbazide and dimethyl acetylenedicarboxylate (DMAD). The structure compound elucidated using various spectral techniques such as FTIR, UV‐spec, 1 H NMR 13 C NMR. related confirmed by single‐crystal X‐ray analysis. Antiproliferative activity evaluated in two human cancer cell lines, HepG2 (liver hepatocellular carcinoma line)...
Sevtap Çağlar Yavuzab, Senem Akkoçc , Burak Tüzünd, Onur Şahine & Emin Saripinara*a Department of Chemistry, Faculty Science, Erciyes University, Kayseri, Turkeyb Veterinary Şefaatli Vocational School, Yozgat Bozok Yozgat, Turkeyc Basic Pharmaceutical Sciences, Pharmacy, Süleyman Demirel Isparta, Turkeyd Sivas Cumhuriyet Sivas, Turkeye Scientific and Technological Research Application Center, Sinop Sinop, Turkey
Abstract The furan‐2,3‐dione 1 and the thiosemicarbazones 2 combine with loss of carbon dioxide water yielding 1‐methylenaminopyrimidine‐2‐thione derivatives 3 in moderate yields (30–60%). Their molecular skeleton is confirmed aid an X‐ray structure determination 3c . Hydrolysis leads to 1‐aminopyrimidine‐2‐thione 5
A set of 1,2,4-triazoles containing a hydrazone moiety was synthesized by oxidative cyclization utilizing molecular iodine under mild conditions. These compounds were evaluated as anticancer agents and their binding mechanism investigated.
In an attempt to identify potential active anticancer agents with low cytotoxic properties and CA inhibitors, a new series of hybrid compounds incorporating imidazole ring hydrazone moiety as part their structure were synthesized by aza-Michael addition reaction followed intramolecular cyclization. The was elucidated using various spectral techniques. Synthesized evaluated for in vitro (prostate cell lines; PC3) inhibitory (hCA I hCA II) activity. Among them, some compound displayed...
A series of imidazole derivatives were synthesized from two-component condensation reaction phenylgloxal monohydrate with guanylhydrazone. They characterized by spectroscopic and analytical techniques. The in vitro anticancer evaluation these compounds was done on human breast cancer (MCF-7) liver (HepG2) cell lines using the MTT assay method. Most newly displayed cytotoxic activity against cancerous cells. In fact, 3a, 3e, 3 h exhibited more activities than positive control drugs, fluro-5,...
Abstract In a single reaction step, pyrimidine derivatives ( 4a‐p ) were synthesized from the triple of aromatic aldehydes 1) , ethyl cyanoacetate 2) and some guanyl hydrazone (3a‐n) . These compounds tested as in vitro against two types cancerous cell lines, namely, human colon line (DLD‐1) breast (MDA‐MB‐231). According to obtained results, nearly all have cytotoxic activity lines. Especially, 4j 4k 4n had significant effect DLD‐1. Furthermore, 4g 4m 4o exhibited lower IC 50 values...
Furan-2,3-diones 1a-c react with various hydrazines 2a-c under different conditions to yield the pyrazole-3-carboxylic acid-hydrazide 3a-d. Cyclocondensation reactions of 1a or 7 phenylhydrazine lead derivatives pyrazolo[3,4-d]pyridazinones 6 and 8, respectively. The structures all products were confirmed by elemental analysis, IR, 1H- 13C-NMR spectroscopic measurements.
The electron conformational-genetic algorithm (EC-GA), a sophisticated hybrid approach combining the GA and EC methods, has been employed for 4D-QSAR procedure to identify pharmacophore benzotriazines as sarcoma inhibitors quantitative prediction of activity. calculated geometry electronic structure parameters every atom bond each molecule are arranged in matrix described electron-conformational contiguity (ECMC). By comparing ECMC one most active compounds with other ECMCs we were able...
In this paper, we present the results of pharmacophore identification and bioactivity prediction for pyrrolo[2,1-c][1,4]benzodiazepine derivatives using electron conformational-genetic algorithm (EC-GA) method as 4D-QSAR analysis. Using data obtained from quantum chemical calculations at PM3/HF level, conformational matrices congruity (ECMC) were constructed by EMRE software. The ECMC lowest energy conformer compound with highest activity was chosen template compared ECMCs other compounds...
Abstract In recent years, various compounds including the aminoguanidine scaffold have been reported to exhibit diverse biological activities. current study, 16 that include guanylhydrazone (aminoguanidine) moiety ( 3 a – p ) were synthesized and characterized through spectrum data, 1 H‐NMR, 13 C‐NMR, FT‐IR. Furthermore, proposed structure of was resolved by single‐crystal X‐ray diffractometer. The prepared then tested for their different in vitro activities antitumor against several types...
The electron conformational and genetic algorithm methods (EC–GA) were integrated for the identification of pharmacophore group predicting anti HIV-1 activity tetrahydroimidazo[4,5,1-jk][1,4]benzodiazepinone (TIBO) derivatives. To reveal group, each conformation all compounds was arranged by matrices congruity. Multiple comparisons these matrices, within given tolerances high active low TIBO derivatives, allow that refers to submatrix activity. effects conformations, internal external...
In this work, the EC–GA method, a hybrid 4D-QSAR approach that combines electron conformational (EC) and genetic algorithm optimization (GA) methods, was applied in order to explain pharmacophore (Pha) predict anti-HIV-1 activity by studying 115 compounds class of 1-[(2-hydroxyethoxy)-methyl]-6-(phenylthio) thymine (HEPT) derivatives as non-nucleoside reverse transcriptase inhibitors (NNRTIs). The series NNRTIs were partitioned into four training test sets from which corresponding...