PubMed İndeksli Yayınlar Koleksiyonu
Permanent URI for this collectionhttps://hdl.handle.net/20.500.14627/8
Browse
2 results
Search Results
Article 1,2,4-Triazole Conjugates as HEGFR Inhibitors: Synthesis, Anticancer Evaluation, and in Silico Studies(Wiley-V C H Verlag GmbH, 2026) Bulbul, Bahadir; Kulabas, Necla; Gurboga, Merve; Ozakpinar, Ozlem Bingol; Cakmak, Ummuhan; Tuncay, Fulya Oz; Kucukguzel, IlkayA series of novel 1,2,4-triazole-acetamide derivatives was synthesized and evaluated for anticancer and hEGFR inhibitory activity. The compounds were obtained via multistep synthesis and characterized by spectroscopic methods. Cytotoxicity was tested against PC-3, MCF-7, A549, and K562 cell lines. Compounds <bold>18</bold>, <bold>19</bold>, and especially <bold>24</bold> showed notable antiproliferative effects, with compound <bold>24</bold> exhibiting higher selectivity and potency than gefitinib. It also induced apoptosis and inhibited migration in A549 and PC-3 cells, while selectively promoting invasion in PC-3, suggesting EMT-related behavior. In vitro kinase assays revealed compound <bold>20</bold> as the most potent hEGFR inhibitor (IC50 = 43.8 +/- 1.3 nM). Molecular docking and 200 ns molecular dynamics simulations confirmed its stable interaction with EGFR, particularly involving Cys797. These findings highlight compounds <bold>20</bold> and <bold>24</bold> as promising candidates for further development as EGFR-targeted anticancer agents.Review Citation - WoS: 7Citation - Scopus: 8Recent Progress on Apoptotic Activity of Triazoles(Bentham Science Publ Ltd, 2021) Cikla-Suzgun, P.; Kucukguzel, S. G.Apoptosis is often called programmed cell death and is defined as a self-directed cell destruction process. It is different from necrosis due to the activation of caspases during this process. Apoptosis is directly related to cancer progression and plays a vital role in carcinogenesis; all cytotoxic drugs and radiation therapy programs initiate apoptosis in tumor cells. Today, studies show that heterocyclic compounds that contain triazole functionality have anticancer activities; triazoles are 5 membered rings, which contain two carbon and three nitrogen atoms. Therefore, many researchers have synthesized these small active compounds as target structures and evaluated their apoptotic activities. The present review describes recent medicinal aspects of triazoles as anticancer agents that have been reported during the past few years. We hope that the bioactivity of triazole derivatives will be beneficial for the rational design of a new generation of small molecule drugs.