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Volume 27
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Article

New 1,3,4-Thiadiazole Derivatives with Anticancer Activity

by
Sara Janowska
1,
Dmytro Khylyuk
1,
Anna Bielawska
2,
Anna Szymanowska
2,
Agnieszka Gornowicz
2,
Krzysztof Bielawski
3,
Jarosław Noworól
4,
Sławomir Mandziuk
5 and
Monika Wujec
1,*
1
Department of Organic Chemistry, Faculty of Pharmacy, Medical University, 4a Chodzki Street, 20-093 Lublin, Poland
2
Department of Biotechnology, Faculty of Pharmacy, Medical University of Bialystok, Kilinskiego 1 Street, 15-089 Bialystok, Poland
3
Department of Synthesis and Technology of Drugs, Faculty of Pharmacy, Medical University of Bialystok, Kilinskiego 1 Street, 15-089 Bialystok, Poland
4
Health Care Institute, State Higher School of Technology and Economics in Jarosław, Czarnieckiego 16 Street, 37-500 Jarosław, Poland
5
Department of Pneumology, Oncology and Allergology, Medical University of Lublin, 8 Jaczewskiego Street, 20-090 Lublin, Poland
*
Author to whom correspondence should be addressed.
Molecules 2022, 27(6), 1814; https://doi.org/10.3390/molecules27061814
Submission received: 10 February 2022 / Revised: 2 March 2022 / Accepted: 8 March 2022 / Published: 10 March 2022
(This article belongs to the Special Issue Novel Design and Synthesis of Anticancer Agents)
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Abstract

We designed and synthesized the 1,3,4-thiadiazole derivatives differing in the structure of the substituents in C2 and C5 positions. The cytotoxic activity of the obtained compounds was then determined in biological studies using MCF-7 and MDA-MB-231 breast cancer cells and normal cell line (fibroblasts). The results showed that in both breast cancer cell lines, the strongest anti-proliferative activity was exerted by 2-(2-trifluorometylophenylamino)-5-(3-methoxyphenyl)-1,3,4-thiadiazole. The IC50 values of this compound against MCF-7 and MDA-MB-231 breast cancer cells were 49.6 µM and 53.4 µM, respectively. Importantly, all new compounds had weaker cytotoxic activity on normal cell line than on breast cancer cell lines. In silico studies demonstrated a possible multitarget mode of action for the synthesized compounds. The most likely mechanism of action for the new compounds is connected with the activities of Caspase 3 and Caspase 8 and activation of BAX proteins.
Keywords: 1,3,4-thiadiazole; cytotoxic activity; breast cancer; docking studies 1,3,4-thiadiazole; cytotoxic activity; breast cancer; docking studies
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MDPI and ACS Style

Janowska, S.; Khylyuk, D.; Bielawska, A.; Szymanowska, A.; Gornowicz, A.; Bielawski, K.; Noworól, J.; Mandziuk, S.; Wujec, M. New 1,3,4-Thiadiazole Derivatives with Anticancer Activity. Molecules 2022, 27, 1814. https://doi.org/10.3390/molecules27061814

AMA Style

Janowska S, Khylyuk D, Bielawska A, Szymanowska A, Gornowicz A, Bielawski K, Noworól J, Mandziuk S, Wujec M. New 1,3,4-Thiadiazole Derivatives with Anticancer Activity. Molecules. 2022; 27(6):1814. https://doi.org/10.3390/molecules27061814

Chicago/Turabian Style

Janowska, Sara, Dmytro Khylyuk, Anna Bielawska, Anna Szymanowska, Agnieszka Gornowicz, Krzysztof Bielawski, Jarosław Noworól, Sławomir Mandziuk, and Monika Wujec. 2022. "New 1,3,4-Thiadiazole Derivatives with Anticancer Activity" Molecules 27, no. 6: 1814. https://doi.org/10.3390/molecules27061814

APA Style

Janowska, S., Khylyuk, D., Bielawska, A., Szymanowska, A., Gornowicz, A., Bielawski, K., Noworól, J., Mandziuk, S., & Wujec, M. (2022). New 1,3,4-Thiadiazole Derivatives with Anticancer Activity. Molecules, 27(6), 1814. https://doi.org/10.3390/molecules27061814

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