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Minas Gerais Research Foundation\u2014Brazil","award":["APQ-00789-22"],"award-info":[{"award-number":["APQ-00789-22"]}]},{"name":"Coordena\u00e7\u00e3o de Aperfei\u00e7oamento de Pessoal de N\u00edvel Superior (CAPES) and the National Institute of Science and Technology in Theranostics and Nanobiotechnology\u2014INCT\u2014Teranano. Minas Gerais Research Foundation\u2014Brazil","award":["305328\/2022-0"],"award-info":[{"award-number":["305328\/2022-0"]}]},{"name":"Coordena\u00e7\u00e3o de Aperfei\u00e7oamento de Pessoal de N\u00edvel Superior (CAPES) and the National Institute of Science and Technology in Theranostics and Nanobiotechnology\u2014INCT\u2014Teranano. Minas Gerais Research Foundation\u2014Brazil","award":["405751\/2023-0"],"award-info":[{"award-number":["405751\/2023-0"]}]},{"name":"Coordena\u00e7\u00e3o de Aperfei\u00e7oamento de Pessoal de N\u00edvel Superior (CAPES) and the National Institute of Science and Technology in Theranostics and Nanobiotechnology\u2014INCT\u2014Teranano. Minas Gerais Research Foundation\u2014Brazil","award":["408208\/2018-0"],"award-info":[{"award-number":["408208\/2018-0"]}]},{"name":"Coordena\u00e7\u00e3o de Aperfei\u00e7oamento de Pessoal de N\u00edvel Superior (CAPES) and the National Institute of Science and Technology in Theranostics and Nanobiotechnology\u2014INCT\u2014Teranano. Minas Gerais Research Foundation\u2014Brazil","award":["CNPq 403193\/2022-2"],"award-info":[{"award-number":["CNPq 403193\/2022-2"]}]},{"name":"Coordena\u00e7\u00e3o de Aperfei\u00e7oamento de Pessoal de N\u00edvel Superior (CAPES) and the National Institute of Science and Technology in Theranostics and Nanobiotechnology\u2014INCT\u2014Teranano. Minas Gerais Research Foundation\u2014Brazil","award":["FAPEMIG CBB-APQ 03613-17"],"award-info":[{"award-number":["FAPEMIG CBB-APQ 03613-17"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>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 \u03bcM 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\u2013mesenchymal 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.<\/jats:p>","DOI":"10.3390\/molecules29184471","type":"journal-article","created":{"date-parts":[[2024,9,20]],"date-time":"2024-09-20T07:38:57Z","timestamp":1726817937000},"page":"4471","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":1,"title":["A Novel Compound from the Phenylsulfonylpiperazine Class: Evaluation of In Vitro Activity on Luminal Breast Cancer Cells"],"prefix":"10.3390","volume":"29","author":[{"ORCID":"https:\/\/orcid.org\/0000-0001-8078-6282","authenticated-orcid":false,"given":"Fernanda Cardoso","family":"da Silva","sequence":"first","affiliation":[{"name":"Laboratory of Genetics and Biotechnology, Institute of Biotechnology, Universidade Federal de Uberl\u00e2ndia, Patos de Minas 38700-002, MG, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-2668-5805","authenticated-orcid":false,"given":"Ana Clara Cassiano","family":"Martinho","sequence":"additional","affiliation":[{"name":"Laboratory of Drug Candidate Synthesis, Institute of Chemistry, Universidade Federal de Uberl\u00e2ndia, Uberl\u00e2ndia 38400-902, MG, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Helen Soares Valen\u00e7a","family":"Ferreira","sequence":"additional","affiliation":[{"name":"Laboratory of Genetics and Biotechnology, Institute of Biotechnology, Universidade Federal de Uberl\u00e2ndia, Patos de Minas 38700-002, MG, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Raoni Pais","family":"Siqueira","sequence":"additional","affiliation":[{"name":"Laboratory of Genetics and Biotechnology, Institute of Biotechnology, Universidade Federal de Uberl\u00e2ndia, Patos de Minas 38700-002, MG, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Vinicius Marques","family":"Arruda","sequence":"additional","affiliation":[{"name":"Laboratory of Genetics and Biotechnology, Institute of Biotechnology, Universidade Federal de Uberl\u00e2ndia, Patos de Minas 38700-002, MG, Brazil"},{"name":"Laboratory of Biochemistry, Institute of Biotechnology, Universidade Federal de Uberl\u00e2ndia, Patos de Minas 38700-002, MG, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-5420-7355","authenticated-orcid":false,"given":"Joyce Ferreira da Costa","family":"Guerra","sequence":"additional","affiliation":[{"name":"Laboratory of Biochemistry, Institute of Biotechnology, Universidade Federal de Uberl\u00e2ndia, Patos de Minas 38700-002, MG, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Maria Laura dos Reis","family":"de Souza","sequence":"additional","affiliation":[{"name":"Laboratory of Drug Candidate Synthesis, Institute of Chemistry, Universidade Federal de Uberl\u00e2ndia, Uberl\u00e2ndia 38400-902, MG, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Emanuelly Silva","family":"Landin","sequence":"additional","affiliation":[{"name":"Laboratory of Drug Candidate Synthesis, Institute of Chemistry, Universidade Federal de Uberl\u00e2ndia, Uberl\u00e2ndia 38400-902, MG, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-1402-2035","authenticated-orcid":false,"given":"Celso de Oliveira","family":"Rezende J\u00fanior","sequence":"additional","affiliation":[{"name":"Laboratory of Drug Candidate Synthesis, Institute of Chemistry, Universidade Federal de Uberl\u00e2ndia, Uberl\u00e2ndia 38400-902, MG, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-7593-1403","authenticated-orcid":false,"given":"Thaise Gon\u00e7alves","family":"de Ara\u00fajo","sequence":"additional","affiliation":[{"name":"Laboratory of Genetics and Biotechnology, Institute of Biotechnology, Universidade Federal de Uberl\u00e2ndia, Patos de Minas 38700-002, MG, Brazil"},{"name":"Laboratory of Nanobiotechnology Prof. Dr. Luiz Ricardo Goulart Filho, Institute of Biotechnology, Universidade Federal de Uberl\u00e2ndia, Uberl\u00e2ndia 38405-302, MG, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2024,9,20]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"229","DOI":"10.3322\/caac.21834","article-title":"Global cancer statistics 2022: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries","volume":"74","author":"Bray","year":"2024","journal-title":"CA A Cancer J. 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