Investigation of anticancer properties of the novel synthesixed pyrrole derivatives as potential tyrosine kinase inhibitors
Başlık:
Investigation of anticancer properties of the novel synthesixed pyrrole derivatives as potential tyrosine kinase inhibitors
Yazar:
Kaya, Meltem, author.
Yazar Ek Girişi:
Fiziksel Tanımlama:
xi, 56 leaves: illustrarions, charts;+ 1 computer laser optical disc.
Özet:
In cancer treatment, chemotherapy has some serious side effects, because it targets active cells which might not be cancer cells. Mouth, hair, nail, bone marrow cells are some examples of active cells. For the reason that chemotherapy has side effects, targeted therapy become more important. Tyrosine kinases are most interested target, because they are necessary for cell growth and metastasis. Active form of tyrosine kinases can cause tumour growth and proliferation, angiogenesis, metastasis and antiapoptotic effects. Based on these vital role of tyrosine kinases, they became more important target in cancer treatment. Pyrrole derivatives have been used chemotherapy drugs for years. Semaxanib and Sunitinib, indole derivatives, are tyrosine kinase inhibitors. The main purpose of this research is to investigate the biologic activities of novel synthesized seven pyrrole derivatives, their activities on migration, apoptosis, cell cycle, and mTOR downstream as a potential tyrosine kinase inhibitor. The results of this research proved that these seven compounds have toxicity on HeLa cells with the IC50 values of 140.60 μM, 382.82 μM, 366.44 μM, 542.00 μM, 255.86 μM, 148.59 μM, 171.40 μM, respectively, but toxicity effects of drugs do not depend on apoptosis mechanism. Beside this, D1 and D3 were able to effect cell cycle by arresting at S phase for D1 and G1 phase for D3. It was demonstrated that D1 and D3 inhibited cell migration. And this inhibition was reported as in a relation with overexpression of p- 4EBP1, inhibition of p-p70S6K (Thr) and p-p70S6K (Shr) proteins. Considering all results, D1 and D3 might be potent inhibitory of metastasis of HeLa cells with respect to its effect on cell cycle, migration, p-4EBP1, p-p70S6K (Ser), and p-p70S6K (Thr) protein levels.
Yazar Ek Girişi:
Tüzel Kişi Ek Girişi:
Tek Biçim Eser Adı:
Thesis (Master)--İzmir Institute of Technology: Chemistry.
İzmir Institute of Technology: Chemistry--Thesis (Master).
Elektronik Erişim:
Access to Electronic Versiyon.