Mehlika Dilek Altıntop, Halil I. Ciftci, Mohamed O. Radwan, Belgin Sever, Zafer Asım Kaplancıklı, Taha F. S. Ali, Ryoko Koga, Mikako Fujita, Masami Otsuka, Ahmet Özdemır,
In an attempt to develop potent antitumor agents, new 1,3,4-thiadiazole derivatives were synthesized and evaluated for their cytotoxic effects on multiple human cancer cell lines, including the K562 chronic myelogenous leukemia cell line that expresses the Bcr-Abl tyrosine kinase. N-(5-Nitrothiazol-2-yl)-2-((5-((4-(trifluoromethyl)phenyl)amino)-1,3,4-thiadiazol-2-yl)thio)acetamide (2) inhibited the Abl protein kinase with an IC50 value of 7.4 µM and showed selective activity against the Bcr-Abl positive ...
Tópico(s): Synthesis and Characterization of Heterocyclic Compounds
2017 - Multidisciplinary Digital Publishing Institute | Molecules
Muhammed Karabacak, Mehlika Dilek Altıntop, Halil I. Ciftci, Ryoko Koga, Masami Otsuka, Mikako Fujita, Ahmet Özdemır,
New pyrazoline derivatives were synthesized and evaluated for their cytotoxic effects on AsPC-1 human pancreatic adenocarcinoma, U87 and U251 human glioblastoma cell lines. 1-[((5-(4-Methylphenyl)-1,3,4-oxadiazol-2-yl)thio)acetyl]-3-(2-thienyl)-5-(4-chlorophenyl)-2-pyrazoline (11) was found to be the most effective anticancer agent against AsPC-1 and U251 cell lines, with IC50 values of 16.8 µM and 11.9 µM, respectively. Tumor selectivity of compound 11 was clearly seen between Jurkat human leukemic ...
Tópico(s): Synthesis and Biological Evaluation
2015 - Multidisciplinary Digital Publishing Institute | Molecules
Belgin Sever, Mehlika Dilek Altıntop, Mohamed O. Radwan, Ahmet Özdemır, Masami Otsuka, Mikako Fujita, Halil I. Ciftci,
Epidermal growth factor receptor (EGFR, also known as HER1) and HER2, prominent members of receptor tyrosine kinase (RTK) superfamily, have been reported as diagnostic or prognostic markers in tumor progression. Based on the importance of molecular hybridization of pyrazoline and thiazole scaffolds in the discovery of potent anticancer agents, new thiazolyl-pyrazoline derivatives (3a-v) were synthesized and screened for their cytotoxic effects on A549 human lung adenocarcinoma, MCF-7 human breast adenocarcinoma ...
Tópico(s): Lung Cancer Treatments and Mutations
2019 - Elsevier BV | European Journal of Medicinal Chemistry
Ebru Zeytün, Mehlika Dilek Altıntop, Belgin Sever, Ahmet Özdemır, Doha El‐Sayed Ellakwa, Zeynep Ocak, Halil I. Ciftci, Masami Otsuka, Mikako Fujita, Mohamed O. Radwan,
After the approval of imatinib, more than 25 antitumor agents targeting kinases have been approved, and several promising candidates are at various stages of clinical evaluation.Due to the importance of the thiazole scaffold in targeted anticancer drug discovery, the goal of this work is to identify new thiazolyl hydrazones as potent ABL1 kinase inhibitors for the management of Chronic Myeloid Leukemia (CML).New thiazolyl hydrazones (2a-p) were synthesized and investigated for their cytotoxic effects ...
Tópico(s): Synthesis and biological activity
2020 - Bentham Science Publishers | Anti-Cancer Agents in Medicinal Chemistry
Belgin Sever, Mehlika Dilek Altıntop, Ahmet Özdemır, Gülşen Akalın Çiftçi, Doha E. Ellakwa, Hiroshi Tateishi, Mohamed O. Radwan, Mahmoud A. A. Ibrahim, Masami Otsuka, Mikako Fujita, Halil I. Ciftci, Taha F. S. Ali,
Epidermal growth factor receptor (EGFR) and cyclooxygenase-2 (COX-2) are crucial targetable enzymes in cancer management. Therefore, herein, new 2-[(5-((1H-indol-3-yl)methyl)-1,3,4-oxadiazol-2-yl)thio]-N-(thiazol/benzothiazol-2-yl)acetamides (2a–i) were designed and synthesized as EGFR and COX-2 inhibitors. The cytotoxic effects of compounds 2a–i on HCT116 human colorectal carcinoma, A549 human lung adenocarcinoma, and A375 human melanoma cell lines were determined using MTT assay. 2-[(5-((1H-Indol- ...
Tópico(s): Synthesis and Biological Evaluation
2020 - Multidisciplinary Digital Publishing Institute | Molecules
Mahmut Fırat Kaynak, İsmail Altıntop, Halil İbrahim ÇIKRIKLAR, Fatma Nurhan Özdemir, Sibel Gafuroğulları, Nizameddin Koca,
Objectives.The personnel of Emergency Service (ES) is under stress due to the intensity of the resulting from the very nature of the work to be performed in this department, which is characterized by the need of providing rapidly medical care to patients with often severe or even life-treating health problem and by though working conditions.In our study, we aimed to determine the satisfaction of resident physicians about choosing the emergency medicine, the factors affecting this satisfaction, and ...
Tópico(s): Emergency Medicine Education and Research
2016 - Turkish Online Journal of Qualitative Inquiry (TOJQI) | The European Research Journal
Halil I. Ciftci, Mohamed O. Radwan, Belgin Sever, Ahmed K. Hamdy, Safiye Emirdağ, Nafia Gökçe Ulusoy, Ece Sözer, Mustafa Can, Nurettin Yaylı, Norie Araki, Hiroshi Tateishi, Masami Otsuka, Mikako Fujita, Mehlika Dilek Altıntop,
Glioma, particularly its most malignant form, glioblastoma multiforme (GBM), is the most common and aggressive malignant central nervous system tumor. The drawbacks of the current chemotherapy for GBM have aroused curiosity in the search for targeted therapies. Aberrantly overexpressed epidermal growth factor receptor (EGFR) in GBM results in poor prognosis, low survival rates, poor responses to therapy and recurrence, and therefore EGFR-targeted therapy stands out as a promising approach for the ...
Tópico(s): Pharmacological Effects of Natural Compounds
2021 - Multidisciplinary Digital Publishing Institute | International Journal of Molecular Sciences
Ahmet Özdemır, Halil I. Ciftci, Belgin Sever, Hiroshi Tateishi, Masami Otsuka, Mikako Fujita, Mehlika Dilek Altıntop,
Non-small cell lung cancer (NSCLC) is the leading cause of cancer-related death throughout the world. Due to the shortcomings of traditional chemotherapy, targeted therapies have come into prominence for the management of NSCLC. In particular, epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) therapy has emerged as a first-line therapy for NSCLC patients with EGFR-activating mutations. In this context, new indenopyrazoles, which were prepared by an efficient microwave-assisted ...
Tópico(s): Quinazolinone synthesis and applications
2022 - Multidisciplinary Digital Publishing Institute | Molecules