N -(5-(Trifluoromethyl)-1,3,4-Thiadiazol-2-Yl)Benzamide and Benzothioamide Derivatives Induce Apoptosis Via Caspase-Dependent Pathway

Alireza Aliabadi; Nazanin-Sadat Afnanzade; Leila Hosseinzadeh; Ahmad Mohammadi-Farani; Mohammad Hossein Shafiee; Hanifeh Nazari; Farahnaz Ahmadi; Alireza Foroumadi

doi:10.1007/s11094-019-02031-x

N-(5-(Trifluoromethyl)-1,3,4-Thiadiazol-2-Yl)Benzamide and Benzothioamide Derivatives Induce Apoptosis Via Caspase-Dependent Pathway

Authors: Aliabadi A.¹^,2, Afnanzade N.²^,3, Hosseinzadeh L.¹^,4, Mohammadi-Farani A.¹^,4, Shafiee M.H.²^,3, Nazari H.³^,4, Ahmadi F.¹^,4, Foroumadi A.⁵
Affiliations:
1. Pharmaceutical Sciences Research Center, School of Pharmacy, Kermanshah University of Medical Sciences
2. Department of Medicinal Chemistry, Faculty of Pharmacy, Kermanshah University of Medical Sciences
3. Student Research Committee, Kermanshah University of Medical Sciences
4. Department of Pharmacology and Toxicology, Faculty of Pharmacy, Kermanshah University of Medical Sciences
5. Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences
Issue: Vol 53, No 6 (2019)
Pages: 521-526
Section: Article
URL: https://journals.rcsi.science/0091-150X/article/view/245841
DOI: https://doi.org/10.1007/s11094-019-02031-x
ID: 245841

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Abstract

New 1,3,4-thiadiazole-based compounds were designed, synthesized, and their anticancer effects were assessed by MTT assay against PC3 (prostate cancer), HT-29 (colon cancer), and SKNMC (neuroblastoma) cell lines. The results were compared to that of doxorubicin. According to MTT assay, some of the synthesized compounds exhibit higher cytotoxic activity (IC ₅₀ , μM range) than doxorubicin against PC3 and SKNMC cells but not HT29 cells. According to the analysis of structure – activity relationship, compounds with methoxy group as an electron donating moiety rendered higher activity than nitro group as an electron withdrawing group. Compound 4d with ortho position of methoxy moiety activated caspases 3 and 9 in both PC3 and HT-29 cell lines.

Keywords

synthesis, bioisosteric change, 1,3,4-thiadiazole, MTT, caspase activity

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N-(5-(Trifluoromethyl)-1,3,4-Thiadiazol-2-Yl)Benzamide and Benzothioamide Derivatives Induce Apoptosis Via Caspase-Dependent Pathway

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