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Article

A Novel Compound from the Phenylsulfonylpiperazine Class: Evaluation of In Vitro Activity on Luminal Breast Cancer Cells

by
Fernanda Cardoso da Silva
1,
Ana Clara Cassiano Martinho
2,
Helen Soares Valença Ferreira
1,
Raoni Pais Siqueira
1,
Vinicius Marques Arruda
1,3,
Joyce Ferreira da Costa Guerra
3,
Maria Laura dos Reis de Souza
2,
Emanuelly Silva Landin
2,
Celso de Oliveira Rezende Júnior
2 and
Thaise Gonçalves de Araújo
1,4,*
1
Laboratory of Genetics and Biotechnology, Institute of Biotechnology, Universidade Federal de Uberlândia, Patos de Minas 38700-002, MG, Brazil
2
Laboratory of Drug Candidate Synthesis, Institute of Chemistry, Universidade Federal de Uberlândia, Uberlândia 38400-902, MG, Brazil
3
Laboratory of Biochemistry, Institute of Biotechnology, Universidade Federal de Uberlândia, Patos de Minas 38700-002, MG, Brazil
4
Laboratory of Nanobiotechnology Prof. Dr. Luiz Ricardo Goulart Filho, Institute of Biotechnology, Universidade Federal de Uberlândia, Uberlândia 38405-302, MG, Brazil
*
Author to whom correspondence should be addressed.
Molecules 2024, 29(18), 4471; https://doi.org/10.3390/molecules29184471
Submission received: 18 July 2024 / Revised: 30 August 2024 / Accepted: 17 September 2024 / Published: 20 September 2024
(This article belongs to the Special Issue Heterocycles: Design, Synthesis and Biological Evaluation, 2nd Edition)
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Abstract

Breast cancer (BC) is the most common cancer in women, and is characterized by its histological and molecular heterogeneity. Luminal BC is an estrogen receptor-positive subtype, with varied clinical courses. Although BC patients are eligible for hormone therapy, both early and late relapses still occur, and thus there is a demand for new cytotoxic and selective treatment strategies for these patients. In the present study, inspired by the structure of phenylsulfonylpiperazine, a series of 20 derivatives were tested in bioassays against MCF7, MDA-MB-231 and MDA-MB-453 BC cells to discover new hit compounds. After 48 h of treatment, 12 derivatives impaired cell viability and presented significant IC50 values against at least one of the tumor lineages. Overall, the luminal BC cell line MCF7 was more sensitive to treatments. Compound 3, (4-(1H-tetrazol-1-yl)phenyl)(4-((4-chlorophenyl)sulfonyl)piperazin-1-yl)methanone, was the most promising, with IC50 = 4.48 μM and selective index (SI) = 35.6 in MCF7 cells. Compound 3 also presented significant antimigratory and antiproliferative activities against luminal BC cells, possibly by affecting the expression of genes involved in the epithelial–mesenchymal transition mechanism, upregulating E-Cadherin transcripts (CDH1). Our findings suggest that phenylsulfonylpiperazine derivatives are potential candidates for the development of new therapies, especially those targeting luminal BC.
Keywords: breast cancer; chemotherapy; phenylsulfonylpiperazine; sulfonamides; cytotoxicity breast cancer; chemotherapy; phenylsulfonylpiperazine; sulfonamides; cytotoxicity

Share and Cite

MDPI and ACS Style

da Silva, F.C.; Martinho, A.C.C.; Ferreira, H.S.V.; Siqueira, R.P.; Arruda, V.M.; Guerra, J.F.d.C.; de Souza, M.L.d.R.; Landin, E.S.; Rezende Júnior, C.d.O.; de Araújo, T.G. A Novel Compound from the Phenylsulfonylpiperazine Class: Evaluation of In Vitro Activity on Luminal Breast Cancer Cells. Molecules 2024, 29, 4471. https://doi.org/10.3390/molecules29184471

AMA Style

da Silva FC, Martinho ACC, Ferreira HSV, Siqueira RP, Arruda VM, Guerra JFdC, de Souza MLdR, Landin ES, Rezende Júnior CdO, de Araújo TG. A Novel Compound from the Phenylsulfonylpiperazine Class: Evaluation of In Vitro Activity on Luminal Breast Cancer Cells. Molecules. 2024; 29(18):4471. https://doi.org/10.3390/molecules29184471

Chicago/Turabian Style

da Silva, Fernanda Cardoso, Ana Clara Cassiano Martinho, Helen Soares Valença Ferreira, Raoni Pais Siqueira, Vinicius Marques Arruda, Joyce Ferreira da Costa Guerra, Maria Laura dos Reis de Souza, Emanuelly Silva Landin, Celso de Oliveira Rezende Júnior, and Thaise Gonçalves de Araújo. 2024. "A Novel Compound from the Phenylsulfonylpiperazine Class: Evaluation of In Vitro Activity on Luminal Breast Cancer Cells" Molecules 29, no. 18: 4471. https://doi.org/10.3390/molecules29184471

APA Style

da Silva, F. C., Martinho, A. C. C., Ferreira, H. S. V., Siqueira, R. P., Arruda, V. M., Guerra, J. F. d. C., de Souza, M. L. d. R., Landin, E. S., Rezende Júnior, C. d. O., & de Araújo, T. G. (2024). A Novel Compound from the Phenylsulfonylpiperazine Class: Evaluation of In Vitro Activity on Luminal Breast Cancer Cells. Molecules, 29(18), 4471. https://doi.org/10.3390/molecules29184471

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