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.


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...
Anti-Cancer Effects of Clofazimine As a Single Agent and in Combination with Cisplatin in Multiple Myeloma
Durusu, Ipek; Hüsnügil, Hepşen Hazal; Atas, Heval; Biber, Aysenur; Gerekci, Selin; Gulec, Aliye Ezgi; Özen, Can (2016-12-02)
Multiple Myeloma (MM) is a malignant neoplasm of bone marrow plasma B cells with high morbidity. Clofazimine (CLF) is an FDA-approved leprostatic, anti-tuberculosis, and anti-inflammatory drug that was previously shown to have growth suppression effect on various cancer types such as hepatocellular, lung, cervix, esophageal, colon, and breast cancer as well as melanoma, neuroblastoma, and leukemia. The objective of this study was to evaluate the anticancer effect and mechanism of CLF on U266 MM cell line. C...
Mutlu, Pelin; Pourianazar, Negar Taghavi; Yucel, Meral; Gündüz, Ufuk (2018-01-01)
Activation of the Wnt signaling in some types of cancer and its relation with chemotherapy resistance is a very interesting issue that has been emphasized in recent years. Although, it is known that increase in the activity of beta-catenin is important in blast transformation and drug resistance, the underlying mechanisms are still unclear. In this study, changes in the expression levels of 186 genes that are thought to be important in drug resistance and Wnt signaling pathways were determined by using qPCR...
Mechanisms of cellular resistance to imatinib in human chronic myeloid leukemia cells
BARAN, YUSUF; Ural, Ali Ugur; Gündüz, Ufuk (2007-12-01)
A major advancement in the treatment of chronic myeloid leukemia (CML) has been the development of imatinib, which has shown striking activity in the chronic phase and the accelerated phase, but less so in the blast phase of the disease. Despite high rates of hematologic and cytogenetic responses to therapy, the emergence of resistance to imatinib has been recognized as a major problem in the treatment of patients with CML.
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.