Design, synthesis and in vitro evaluation of new thiosemicarbazone derivatives as potential anticancer agents

Belgin Sever; Gülşen Akalın Çiftçi; Ahmet Özdemir; Mehlika Dilek Altıntop

Design, synthesis and in vitro evaluation of new thiosemicarbazone derivatives as potential anticancer agents

Abstract

Thiosemicarbazones play a pivotal role as potential therapeutic agents for the management of lung cancer. 4-(4-Cyanophenyl)-1-[(5-arylfuran-2-yl)methylene]thiosemicarbazides (1-10) were obtained via the reaction of 4-(4 cyanophenyl)thiosemicarbazide with 5-arylfurfurals. MTT assay was performed to assess their cytotoxic effects on A549 human lung adenocarcinoma and L929 mouse fibroblast cell lines. Compounds 1, 5, 6 and 7 were identified as the most effective anticancer agents on A549 cell line with IC50 values of 12.75±0.35 µg/mL, 4.30±0.61 µg/mL, 5.50±2.12 µg/mL and 5.90±0.57 µg/mL, respectively compared to cisplatin (IC50= 12.00±0.71 µg/mL). The IC50 values of these compounds for L929 cell line were higher than their IC50 values for A549 cell line indicating that their anticancer effects were selective. The apoptotic effects of these compounds were also analyzed based on Annexin V-PI binding capacities in flow cytometry. According to flow cytometric analyses, the early apoptotic effects of compounds 1, 5, 6 and 7 on A549 cell line were determined as 4.7, 5.1, 7.3 and 5.1%, whereas their late apoptotic effects were determined as 3.7, 2.0, 4.9 and 3.3%, respectively. Compound 6 showed more apoptotic activity than compounds 1, 5 and 7. According to these findings, compounds 5 and 6 stand out as promising anticancer agents for further in vitro and in vivo studies.

Keywords

References

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Details

Primary Language

English

Subjects

Pharmaceutical Biochemistry, Pharmaceutical Chemistry

Journal Section

Research Article

Authors

Belgin Sever
Türkiye

Gülşen Akalın Çiftçi
Türkiye

Ahmet Özdemir
Türkiye

Mehlika Dilek Altıntop ^*
Türkiye

Publication Date

June 27, 2025

Submission Date

June 1, 2018

Acceptance Date

August 31, 2018

Published in Issue

Year 2019 Volume: 23 Number: 1

IZ

https://izlik.org/JA77XK38UM

Cite

RIS / Bibtex

APA

Sever, B., Akalın Çiftçi, G., Özdemir, A., & Altıntop, M. D. (2025). Design, synthesis and in vitro evaluation of new thiosemicarbazone derivatives as potential anticancer agents. Journal of Research in Pharmacy, 23(1), 16-24. https://izlik.org/JA77XK38UM

AMA

1.Sever B, Akalın Çiftçi G, Özdemir A, Altıntop MD. Design, synthesis and in vitro evaluation of new thiosemicarbazone derivatives as potential anticancer agents. J. Res. Pharm. 2025;23(1):16-24. https://izlik.org/JA77XK38UM

Chicago

Sever, Belgin, Gülşen Akalın Çiftçi, Ahmet Özdemir, and Mehlika Dilek Altıntop. 2025. “Design, Synthesis and in Vitro Evaluation of New Thiosemicarbazone Derivatives As Potential Anticancer Agents”. Journal of Research in Pharmacy 23 (1): 16-24. https://izlik.org/JA77XK38UM.

EndNote

Sever B, Akalın Çiftçi G, Özdemir A, Altıntop MD (June 1, 2025) Design, synthesis and in vitro evaluation of new thiosemicarbazone derivatives as potential anticancer agents. Journal of Research in Pharmacy 23 1 16–24.

IEEE

[1]B. Sever, G. Akalın Çiftçi, A. Özdemir, and M. D. Altıntop, “Design, synthesis and in vitro evaluation of new thiosemicarbazone derivatives as potential anticancer agents”, J. Res. Pharm., vol. 23, no. 1, pp. 16–24, June 2025, [Online]. Available: https://izlik.org/JA77XK38UM

ISNAD

Sever, Belgin - Akalın Çiftçi, Gülşen - Özdemir, Ahmet - Altıntop, Mehlika Dilek. “Design, Synthesis and in Vitro Evaluation of New Thiosemicarbazone Derivatives As Potential Anticancer Agents”. Journal of Research in Pharmacy 23/1 (June 1, 2025): 16-24. https://izlik.org/JA77XK38UM.

JAMA

1.Sever B, Akalın Çiftçi G, Özdemir A, Altıntop MD. Design, synthesis and in vitro evaluation of new thiosemicarbazone derivatives as potential anticancer agents. J. Res. Pharm. 2025;23:16–24.

MLA

Sever, Belgin, et al. “Design, Synthesis and in Vitro Evaluation of New Thiosemicarbazone Derivatives As Potential Anticancer Agents”. Journal of Research in Pharmacy, vol. 23, no. 1, June 2025, pp. 16-24, https://izlik.org/JA77XK38UM.

Vancouver

1.Belgin Sever, Gülşen Akalın Çiftçi, Ahmet Özdemir, Mehlika Dilek Altıntop. Design, synthesis and in vitro evaluation of new thiosemicarbazone derivatives as potential anticancer agents. J. Res. Pharm. [Internet]. 2025 Jun. 1;23(1):16-24. Available from: https://izlik.org/JA77XK38UM