Altintop Mehlika Dilek, Sever Belgin, Özdemir Ahmet, Kuş Gökhan, Oztopcu-Vatan Pinar, Kabadere Selda, Kaplancikli Zafer Asim
a Department of Pharmaceutical Chemistry, Faculty of Pharmacy , Anadolu University , Eskişehir , Turkey .
b Open Education Faculty , Anadolu University , Eskişehir , Turkey .
J Enzyme Inhib Med Chem. 2016;31(3):410-6. doi: 10.3109/14756366.2015.1031126. Epub 2015 Mar 31.
Fourteen new naphthalene-based thiosemicarbazone derivatives were designed as anticancer agents against LNCaP human prostate cancer cells and synthesized. MTT assay indicated that compounds 6, 8 and 11 exhibited inhibitory effect on LNCaP cells. Among these compounds, 4-(naphthalen-1-yl)-1-[1-(4-hydroxyphenyl)ethylidene)thiosemicarbazide (6), which caused more than 50% death on LNCaP cells, was chosen for flow cytometric analysis of apoptosis. Flow cytometric analysis pointed out that compound 6 also showed apoptotic effect on LNCaP cells. Compound 6 can be considered as a promising anticancer agent against LNCaP cells owing to its potent cytotoxic activity and apoptotic effect.
设计并合成了14种新型萘基硫代氨基脲衍生物作为抗人LNCaP前列腺癌细胞的抗癌剂。MTT法检测表明，化合物6、8和11对LNCaP细胞具有抑制作用。在这些化合物中，选择对LNCaP细胞造成50%以上死亡的4-(萘-1-基)-1-[1-(4-羟基苯基)亚乙基]硫代氨基脲(6)进行凋亡的流式细胞术分析。流式细胞术分析指出，化合物6对LNCaP细胞也具有凋亡作用。化合物6因其强大的细胞毒活性和凋亡作用，可被认为是一种有前景的抗LNCaP细胞的抗癌剂。
