Studies directed towards The synthesis Of İmatinib Mesylate ((Gleevec), 4-(4-Methyl-Piperazin-1- Ylmethyl)-N-[4- Methyl-3-(4-Pyridin-3-Yl-Pyrimidin-2- Ylamino)-Phenyl]- Benzamide Methanesulfonate) Analogs

Günay, Neşet Batuhan
Imatinib mesylate is indicated for the treatment of chronic myeloid leukemia (CML) and unresectable and/or metastatic malignant gastrointestinal stromal tumors (GIST). By the application of this anticancer drug, problems occurs in terms of stability and activity. Computer assisted design (CAD) works showed that the modification of the B and C part molecule can increase the effectivity of the drug. The new derivatives of the drug will be obtained to change some part of the B and C segments. The total synthesis of a new imatinib mesylate will be done and the activity tests are going to be determined in collaboration with other groups.


Multidrug resistance mechanisms in imatinib resistant human chronic myeloid leukemia cells
Baran, Yusuf; Gündüz, Ufuk; Department of Biology (2006)
In this study, mechanisms of resistance to Imatinib-induced apoptosis in human K562 and Meg-1 chronic myeloid leukemia (CML) cells were examined. Continuous exposure of cells to step-wise increasing concentrations of Imatinib resulted in the selection of 0.2 and 1 ́M İmatinib resistant cells. Measurement of endogenous ceramide levels showed that treatment with Imatinib increased the generation of C18-ceramide significantly, which is mainly synthesized by the human longevity assurance gene 1 (hLASS1), in sen...
Apoptotic Effects of Resveratrol, a Grape Polyphenol, on Imatinib-Sensitive and Resistant K562 Chronic Myeloid Leukemia Cells
Can, Geylani; Cakir, Zeynep; Kartal, Melts; Gündüz, Ufuk; BARAN, YUSUF (2012-07-01)
Aim: To examine the antiproliferative and apoptotic effects of resveratrol on imatinib-sensitive and imatinib-resistant K562 chronic myeloid leukemia cells. Materials and Methods: Antiproliferative effects of resveratrol were determined by the 3-Bis[2-methoxy-4-nitro-5-sulphophenyl]-2H-tetrazolium-5-carboxanilide inner salt (XTT) cell proliferation assay. Apoptotic effects of resveratrol on sensitive K562 and resistant K562/IMA-3 cells were determined through changes in caspase-3 activity, loss of mitochond...
The low frequency of defective TPMT alleles in Turkish population: A study on pediatric patients with acute lymphoblastic leukemia
Tumer, Tugba Boyunegmez; Ulusoy, Gulen; Adalı, Orhan; Sahin, Gurses; Gozdasoglu, Sevgi; Arinc, Ennel (Wiley, 2007-10-01)
6-Mercaptopurine (6MP) is an essential anticancer drug used in the treatment of childhood acute lymphoblastic leukemia (ALL). Thiopurine methyltransferase (TPMT) polymorphisms are the major determinants of interindividual differences in the severe toxicity or efficacy of 6MP Four variant alleles, TPMT*2, TPMT*3A, TPMT*3B, and TPMT*3C, are responsible over the 80% of low or undetectable enzyme activity. The frequencies of these variants were investigated among 106 children with ALL in Turkish population. TPM...
Identification of polymorphisms on the MDR1 gene among Turkish population and their effects on multidrug resistance in acute leukemia patients
Kaya, P; Gündüz, Ufuk; Arpaci, F; Ural, AU; Guran, S (2005-09-01)
Multidrug-resistance (MDR) phenotype is a serious limitation to the effective chemotherapeutic treatment of many cancer types, including leukemia. One of the most important proteins, the over-expression of which is responsible for the multidrug-resistance phenotype in many cancer types, is P-glycoprotein. This protein is the product of the MDR1 gene. In previous studies, single-nucleotide polymorphisms (SNPs) C3435T, G2677T, and T-129C in the MDR1 gene were shown to be correlated with lower P-glycoprotein e...
Gerekci Yeşilyurt, Selin; Özen, Can; Özçubukçu, Salih; Department of Biochemistry (2022-8-29)
Acute Myeloid Leukemia is a hematological cancer with high phenotypic and genotypic heterogeneity. Patients diagnosed with AML are categorized into risk groups based on cytogenetic and molecular abnormality tests, which determine the specific treatment regimes. Since risk status determination takes significant amount of time and some emergency patients require immediate treatment, a method to provide fast clinical data that will be the basis for initial treatment regime is needed in the medical commun...
Citation Formats
N. B. Günay, “Studies directed towards The synthesis Of İmatinib Mesylate ((Gleevec), 4-(4-Methyl-Piperazin-1- Ylmethyl)-N-[4- Methyl-3-(4-Pyridin-3-Yl-Pyrimidin-2- Ylamino)-Phenyl]- Benzamide Methanesulfonate) Analogs,” M.S. - Master of Science, Middle East Technical University, 2008.