Browsing by Author "Yelekçi, Kemal"
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Nörodejeneratif Hastalıkların önlemesine yönelik In Silico nöronal Nitrik oksit sentaz nnos seçimli inhibitör tasarımı
Yelekçi, Kemal; Kayrak, Nurdan (2013)[Abstract Not Available] -
Pharmacophore-based virtual screening for identification of potential selective inhibitors of human histone deacetylase 6
Uba, Abdullahi Ibrahim; Yelekçi, Kemal (Elsevier Sci Ltd, 2018)Histone deacetylase (HDAC) 6 plays a role in oncogenic transformation and cancer metastasis via tubulin deacetylation, making it a critical target for anticancer drug design. However, lack of selectivity shown by many of ... -
Potent inhibitors designed for methionine aminopeptidase II using pharmocophore modeling /
Bayatı, Safanah A. Al; Yelekçi, Kemal (Kadir Has Üniversitesi, 2019)Metaloenzimlerden Metiyonin Aminopeptidazlar (MetAP2), yeni sentezlenmiş polipep-titlerin başından metionin amino asidini kesmekle sorumludur. MetAP2'nin seçimli olarak engellenmesi damar oluşumunu baskıladığını, katı ... -
Potential inhibitors of methionine aminopeptidase type II identified via structure-based pharmacophore modeling
Albayati, Safana; Uba, Abdullahi İbrahim; Yelekçi, Kemal (Springer Science and Business Media Deutschland GmbH, 2021)Methionine aminopeptidase (MetAP2) is a metal-containing enzyme that removes initiator methionine from the N-terminus of a newly synthesized protein. Inhibition of the enzyme is crucial in diminishing cancer growth and ... -
Power of inhibition activity screening and 3D molecular modeling approaches in HDAC 8 inhibitor design
Tatar, Gamze Bora; Tokluman, Tenzile Deniz; Yelekçi, Kemal; Yurter, Hayat (Scientific Technical Research Council Turkey-Tubitak, 2011)In-vitro inhibition activity screening and in-silico 3D molecular modeling approaches are important tools for design and development of specific histone deacetylase (HDAC) inhibitors. The objective of this study was to ... -
Repurposing of existing drugs for treatment of Covid-19 target RNA-dependent RNA polymerase (RdRp) enzyme-using in silico screening techniques
Kiliç, Meltem (Kadir Has Üniversitesi, 2021)Korona virüsü 2019'dan bu yana dünya genelinde 5 milyondan fazla insanın hayatını kaybetmesine neden olan hastalıktır. 2020 yılında dünya sağlık örgütü tarafından pandemi oluşturan hastalıklar arasına adını yazdıran korona ... -
Structure Prediction of TB RPOB and its Mutations Binding Analysis
Dinçer, Erçin (Kadir Has Üniversitesi, 2012)--Today Tuberculosis is a disease that is still a high-risk categories. Rifampicin is a drug that.s used common in the treatment of TB. We know that the effect of this drug in the region of RNA polymerase on TB. Unfortunately ... -
Synthesis and molecular modeling of some novel hexahydroindazole derivatives as potent monoamine oxidase inhibitors
Gökhan-Kelekçi, Nesrin; Şimşek, O. Özgün; Ercan, Ayşe; Yelekçi, Kemal; Şahin, Z. Sibel; Işık, Şamil; Uçar, Gülberk; Bilgin, Abdullah Altan (Pergamon-Elsevier Science Ltd, 2009)A novel series of 2-thiocarbamoyl-234567-hexahydro-1H-indazole and 2-substituted thiocarbamoyl-33a 4567-hexahydro-2H-indazoles derivatives were synthesized and investigated for the ability to inhibit the activity of the A ... -
Synthesis and screening of hMAO inhibitory activities of some new 2-pyrazoline and hydrazone derivatives
Evranos-Aksoz, Begum; Yabanoglu-Ciftci, Samiye; Ucar, Gulberk; Yelekçi, Kemal; Ertan, Rahmiye (Wiley-Blackwell, 2014)[Abstract Not Available] -
Synthesis and Screening of Human Monoamine Oxidase-A Inhibitor Effect of New 2-Pyrazoline and Hydrazone Derivatives
Evranos-Aksoz, Begüm; Baysal, İpek; Yabanoğlu-Çiftçi, Samiye; Djikic, Teodora; Yelekçi, Kemal; Uçar, Gülberk; Ertan, Rahmiye (Wiley-VCH Verlag GmbH, 2015)A group of 35-diaryl-2-pyrazoline and hydrazone derivatives was prepared via the reaction of various chalcones with hydrazide compounds in ethanol. Twenty original compounds were synthesized. Ten of these original compounds ... -
Synthesis anticancer activity and molecular modeling of etodolac-thioether derivatives as potent methionine aminopeptidase (type II) inhibitors
Çoruh, Işıl; Çevik, Ozge; Yelekçi, Kemal; Djikic, Teodora; Küçükgüzel, Şükriye Güniz (Wiley, 2018)A series of (RS)-1-{[5-(substituted)sulfanyl-4-substituted-4H-124-triazole-3-yl]methyl}-18-diethyl-1349-tetrahydropyrano[34-b]indoles (5a-v) were designed and synthesized using a five-step synthetic protocol that involves ... -
Synthesis Molecular Docking and Anticancer Activity of Diflunisal Derivatives as Cyclooxygenase Enzyme Inhibitors
Coşkun, Göknil Pelin; Djikic, Teodora; Hayal, Taha Bartu; Turkel, Nezaket; Yelekçi, Kemal; Sahin, Fikrettin; Küçükgüzel, Şükriye Güniz (MDPI, 2018)Cyclooxygenase enzymes play a vital role in inflammatory pathways in the human body. Apart from their relation with inflammation the additional involvement of COX-2 enzyme with cancer activity was recently discovered. In ... -
Synthesis molecular modeling and in vitro screening of monoamine oxidase inhibitory activities of some novel hydrazone derivatives
Salgin-Goksen, Umut; Gokhan-Kelekçi, Nesrin; Yabanoglu-Ciftci, Samiye; Yelekçi, Kemal; Ucar, Gulberk (SPRINGER WIEN, 2013)Thirteen 2-[2-(5-methyl-2-benzoxazolinone-3-yl)acetyl]-3/4/5-substituted benzylidenehydrazine derivatives were synthesized by reacting 2-(5-methyl-2-benzoxazolinone-3-yl)acetylhydrazine and substituted benzaldehydes in ... -
Synthesis molecular modeling in vivo study and anticancer activity of 124-triazole containing hydrazide-hydrazones derived from (S)-naproxen
Han, Muhammed İhsan; Bekçi, Hatice; Uba, Abdullahi İbrahim; Yıldırım, Yeliz; Karasulu, Ercüment; Cumaoğlu, Ahmet; Karasulu, Hatice Y.; Yelekçi, Kemal; Yılmaz, Ozguer; Küçükgüzel, Şükriye Güniz (Wiley-VCH Verlag GmbH, 2019)A new series of 124-triazole containing hydrazide-hydrazones derived from (S)-naproxen (7a-m) was synthesized in this study. The structures of these compounds were characterized by spectral (Fourier-transform infrared ... -
Synthesis Molecular Modelling and Antibacterial Activity Against Helicobacter pylori of Novel Diflunisal Derivatives as Urease Enzyme Inhibitors
Coşkun, Göknil Pelin; Djikic, Teodora; Kalaycı, Sadık; Yelekçi, Kemal; Şahin, Fikrettin; Küçükgüzel, Şükriye Güniz (Bentham Science Publ Ltd, 2019)Background: The main factor for the prolongation of the ulcer treatment in the gastrointestinal system would be Helicobacter pylori infection which can possibly lead to gastrointestinal cancer. Triple therapy is the treatment ... -
Synthesis of some novel hydrazone and 2-pyrazoline derivatives: Monoamine oxidase inhibitory activities and docking studies
Evranos-Aksoz, Begum; Yabanoglu-Ciftci, Samiye; Ucar, Gulberk; Yelekçi, Kemal; Ertan, Rahmiye (Pergamon-Elsevier Science Ltd, 2014)A novel series of 2-pyrazoline and hydrazone derivatives were synthesized and investigated for their human monoamine oxidase (hMAO) inhibitory activity. All compounds inhibited the hMAO isoforms (MAO-A or MAO-B) competitively ... -
Synthesis, Anticancer Activity on Prostate Cancer Cell Lines and Molecular Modeling Studies of Flurbiprofen-Thioether Derivatives as Potential Target of MetAP (Type II)
Yılmaz, Özgür; Bayer, Burak; Bekçi, Hatice; Uba, Abdullahi, I; Cumaoğlu, Ahmet; Yelekçi, Kemal; Küçükgüzel, S. Guniz (Bentham Science PUBL LTD, 2020)Background: Prostate cancer is still one of the serious causes of mortality and morbidity in men. Despite recent advances in anticancer therapy, there is a still need of novel agents with more efficacy and specificity in ... -
Synthesis, in silico studies and cytotoxicity evaluation of novel 1,3,4-oxadiazole derivatives designed as potential mPGES-1 inhibitors
Erensoy, Gizem; Ding, Kai; Zhan, Chang-Guo; Elmezayen, Ammar D.; Yelekçi, Kemal; Duracık, Merve; Özakpınar, Özlem Bingol; Küçükgüzel, İlkay (MARMARA UNIV, 2020)A series of new 1,3,4-oxadizole derivatives containing thioether group, has been synthesized to investigate their mPGES-1 inhibitory activities. The synthesized compounds were also evaluated for their anticancer and COX-1/2 ... -
Synthesis, molecular modeling, in vivo study and anticancer activity against prostate cancer of (+) (S)-naproxen derivatives
Uba, Abdullahi Ibrahim; Karasulu, Hatice Yeşim; Karasulu, Ercüment; Birgül, Kaan; Yıldırım, Yeliz; Bekçi, Hatice; Cumaoğlu, Ahmet; Yılmaz, Özgür; Kabasakal, Levent; Küçükgüzel, Şükriye Güniz; Yelekçi, Kemal (Elsevier Masson s.r.l., 2020)In this study, (S)-naproxen thiosemicarbazides (3a-d), 1,2,4-triazoles (4a-c), triazole-thioether hybride compounds (5a-p) were synthesized and their structures (3a, 3d, 4a and 5a-p) were confirmed by FT-IR, 1H NMR,13C ... -
Targeting cancer epigenetic modifiers: The design of isoform-selective histone deacetylase inhibitors
Uba, Abdullahi İbrahim (Kadir Has Üniversitesi, 2018)Epigenetic alterations are believed to be the common hallmark of human cancers. Histone deacetylase (HDAC) inhibitors have proven to be effective in cancer cases where HDACs are up-regulated. However lack of selectivity ...