The Novel Synthesized Pyridazinone Derivates Had the Antiproliferative and Apoptotic Effects in SHSY5Y and HEP3B Cancer Cell Line

被引:4
作者
Ciftci, Osman [1 ]
Ozdemir, Zeynep [2 ]
Acar, Ceren [3 ]
Sozen, Mert [3 ]
Basak-Turkmen, Nese [4 ]
Ayhan, Idris [1 ]
Gozukara, Harika [5 ]
机构
[1] Inonu Univ, Fac Med, Dept Med Pharmacol, TR-44280 Malatya, Turkey
[2] Inonu Univ, Fac Pharm, Dept Pharmaceut Chem, TR-44280 Malatya, Turkey
[3] Inonu Univ, Fac Art & Sci, Dept Mol Biol & Genet, TR-44280 Malatya, Turkey
[4] Inonu Univ, Fac Pharm, Dept Pharmaceut Toxicol, TR-44280 Malatya, Turkey
[5] Inonu Univ, Fac Med, Dept Biostat, TR-44280 Malatya, Turkey
关键词
Apoptotic effects; antitumoral effects; brain cancer; cytotoxic effects; liver cancer; pyridazinone; INHIBITORS;
D O I
10.2174/1570178614666170707154210
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Background: Brain cancer (neuroblastoma) and liver cancer (hepatocellular carcinoma) are common cancer types among others worldwide which do not have a radical treatment and cure. Objective: In the current study, five novel pyridazinone derivates bearing benzelhydrazone moiety at second position were synthesized and evaluated for their cytotoxic activity against neuroblastoma and hepatocellular carcinoma (SHSY5Y and HEP3B) and human fibroblast (HF) cell lines. The aim of the current study is to identify antiproliferative activity of five novel pyridazinone derivates against neuroblastoma and hepatocellular carcinoma (SHSY5Y and HEP3B) and human fibroblast (HF) cell lines. Method: The compounds were synthesized by the reacting 6-[4-(phenyl/4-chlorophenyl)piperazine-1yl]-3(2H)-pyridazinone-2-yl acetohydrazide with benzaldehyde in ethanol. The in vitro antiproliferative activities were determined with MTT assay. Bax, Bcl-2 and Casp3 gene expression levels were detected with RT-PCR analyses. Results: The lowest IC50 was observed for compound 4 in SHSY5Y and HEP3B cells. Apoptosis increased in cancer cells which was shown by changes inBax, Bcl-2 and Casp3 gene expression levels with 1-5 compound therapy. Conclusion: Novel pyridazinone derivates might be promising agents as new chemotherapeutic candidates in brain and liver cancer.
引用
收藏
页码:323 / 331
页数:9
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