Literature DB >> 24123162

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.

Leila Hosseinzadeh1, Amanc Khorand, Alireza Aliabadi.   

Abstract

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.
© 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Entities:  

Keywords:  1,3,4-Thiadiazole; Anticancer; Apoptosis; Caspase enzymes; Synthesis

Mesh:

Substances:

Year:  2013        PMID: 24123162     DOI: 10.1002/ardp.201300180

Source DB:  PubMed          Journal:  Arch Pharm (Weinheim)        ISSN: 0365-6233            Impact factor:   3.751


  14 in total

1.  Comprehensive Study on Thiadiazole-Based Anticancer Agents Inducing Cell Cycle Arrest and Apoptosis/Necrosis Through Suppression of Akt Activity in Lung Adenocarcinoma and Glioma Cells.

Authors:  Gülşen Akalin Çiftçi; Belgin Sever; Mehlika Dilek Altintop
Journal:  Turk J Pharm Sci       Date:  2019-03-27

2.  Encapsulation in PLGA-PEG enhances 9- nitro-camptothecin cytotoxicity to human ovarian carcinoma cell line through apoptosis pathway.

Authors:  F Ahmadi; K Derakhshandeh; A Jalalizadeh; A Mostafaie; L Hosseinzadeh
Journal:  Res Pharm Sci       Date:  2015 Mar-Apr

3.  Comparative Evaluation of Cytotoxic and Apoptogenic Effects of Several Coumarins on Human Cancer Cell Lines: Osthole Induces Apoptosis in p53-Deficient H1299 Cells.

Authors:  Yalda Shokoohinia; Leila Hosseinzadeh; Maryam Alipour; Ali Mostafaie; Hamid-Reza Mohammadi-Motlagh
Journal:  Adv Pharmacol Sci       Date:  2014-09-03

4.  Protective effects of fractions from Artemisia biennis hydro-ethanolic extract against doxorubicin-induced oxidative stress and apoptosis in PC12 cells.

Authors:  Mahdi Mojarrab; Mehran Mehrabi; Farahnaz Ahmadi; Leila Hosseinzadeh
Journal:  Iran J Basic Med Sci       Date:  2016-05       Impact factor: 2.699

5.  Evaluation of antioxidant and cytoprotective activities of Artemisia ciniformis extracts on PC12 cells.

Authors:  Mahdi Mojarrab; Sajjad Nasseri; Leila Hosseinzadeh; Farah Farahani
Journal:  Iran J Basic Med Sci       Date:  2016-04       Impact factor: 2.699

6.  Synthesis and Biological Evaluation of N-(5-(pyridin-2-yl)-1,3,4-thiadiazol-2-yl)benzamide Derivatives as Lipoxygenase Inhibitor with Potential Anticancer Activity.

Authors:  Alireza Aliabadi; Ahmad Mohammadi-Farani; Sahar Roodabeh; Farahnaz Ahmadi
Journal:  Iran J Pharm Res       Date:  2017       Impact factor: 1.696

7.  Design, Synthesis, and Biological Evaluation of Novel 1,3,4-Thiadiazole Derivatives as Potential Antitumor Agents against Chronic Myelogenous Leukemia: Striking Effect of Nitrothiazole Moiety.

Authors:  Mehlika Dilek Altıntop; Halil Ibrahim Ciftci; Mohamed O Radwan; Belgin Sever; Zafer Asım Kaplancıklı; Taha F S Ali; Ryoko Koga; Mikako Fujita; Masami Otsuka; Ahmet Özdemir
Journal:  Molecules       Date:  2017-12-27       Impact factor: 4.411

8.  A semipolar fraction of petroleum ether extract of Artemisia aucheri induces apoptosis and enhances the apoptotic response to doxorubicin in human neuroblastoma SKNMC cell line.

Authors:  Farahnaz Ahmadi; Mahdi Mojarrab; Mahmoud Ghazi-Khansari; Leila Hosseinzadeh
Journal:  Res Pharm Sci       Date:  2015 Jul-Aug

9.  Osthole attenuates doxorubicin-induced apoptosis in PC12 cells through inhibition of mitochondrial dysfunction and ROS production.

Authors:  Yalda Shokoohinia; Leila Hosseinzadeh; Maryam Moieni-Arya; Ali Mostafaie; Hamid-Reza Mohammadi-Motlagh
Journal:  Biomed Res Int       Date:  2014-06-12       Impact factor: 3.411

10.  Bioassay-guided Isolation of Neuroprotective Fatty Acids from Nigella sativa against 1-methyl-4-phenylpyridinium-induced Neurotoxicity.

Authors:  Leila Hosseinzadeh; Hoda Monaghash; Farahnaz Ahmadi; Nastaran Ghiasvand; Yalda Shokoohinia
Journal:  Pharmacogn Mag       Date:  2017-11-13       Impact factor: 1.085

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