Discovery of 2-Phenyl-N-(5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl)acetamide Derivatives as Apoptosis Inducers via the Caspase Pathway with Potential Anticancer Activity

被引:34
作者
Hosseinzadeh, Leila [1 ]
Khorand, Amanc [2 ,3 ]
Aliabadi, Alireza [3 ]
机构
[1] Kermanshah Univ Med Sci, Dept Pharmacol Toxicol & Med Serv, Fac Pharm, Kermanshah, Iran
[2] Kermanshah Univ Med Sci, Students Res Comm, Kermanshah, Iran
[3] Kermanshah Univ Med Sci, Dept Med Chem, Fac Pharm, Kermanshah, Iran
关键词
Anticancer; Apoptosis; Caspase enzymes; Synthesis; 1,3,4-Thiadiazole; CANCER; 1,3,4-THIADIAZOLES; INHIBITORS;
D O I
10.1002/ardp.201300180
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
In the current research of medicinal chemistry, apoptosis induction is one of the novel strategies for the development and discovery of novel anticancer therapeutics. In the present study, a new series of 1,3,4-thiadiazole derivatives (4a-4p) were synthesized and their in vitro anticancer activities were evaluated against three cancer cell lines: PC3 (prostate cancer), MCF7 (breast cancer), and SKNMC (neuroblastoma). These cell lines were utilized in MTT assays and the obtained results were compared to doxorubicin. Apoptosis induction was also investigated through exploration of the activation of caspases 3, 8, and 9. According to the obtained results, compounds 4b (3-Cl) and 4c (4-Cl) demonstrated the best caspase activation. In fact, compounds 4b and 4c enhanced the activity of caspases 3 and 9 in the MCF7 cell line.
引用
收藏
页码:812 / 818
页数:7
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