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. Issue 11 (1st October 2013)

• Record Type: Journal Article
• Authors: Hosseinzadeh, Leila; Khorand, Amanc; Aliabadi, Alireza
• Is Part Of: Archiv der Pharmazie. Volume 346:Issue 11(2013:Nov.)
• Page Start: 812
• Page End: 818
• Publication Date: 2013-10-01
• Subjects: Pharmaceutical chemistry -- Periodicals; Pharmacology -- Periodicals; 615.19
• DOI: 10.1002/ardp.201300180
• Languages: English
• ISSNs: 0365-6233

Abstract

<abstract abstract-type="main" xml:lang="en"> <title>Abstract</title> <sec id="ardp201300180-sec-0001" sec-type="section"> <p>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 (<bold>4a–4p</bold>) were synthesized and their <italic>in vitro</italic> 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 <bold>4b</bold> (3‐Cl) and <bold>4c</bold> (4‐Cl) demonstrated the best caspase activation. In fact, compounds <bold>4b</bold> and <bold>4c</bold> enhanced the activity of caspases 3 and 9 in the MCF7 cell line.</p> </sec> </abstract>