title: Targeting triple-negative breast cancer cells with 6,7-bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoles.
abstract: Further studies on 6,7-bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoles as anticancer agents against breast cancer are reported, allowing to demonstrate the potential of these compounds for the therapy of the triple-negative breast cancer, the most challenging tumors in clinical practice. These compounds were assayed for their in vitro cytotoxicity on several human breast cancer cell lines (MCF7, HCC1954 and HCC1806 cell lines). Particularly interesting were the results obtained for 4-hydroxyphenyl substituted derivative, which proved to be the most promising compound regarding HCC1806 cell line, a triple-negative breast cancer. The effects of the two most active compounds on cell survival, viability, cell cycle, DNA damage and expression of proteins related to cell death pathways were studied. The reported results consolidate the potential of 6,7-bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoles for the therapy of breast cancer, particularly the triple-negative.
authors.affiliation: Biophysics Unit, Faculty of Medicine of University of Coimbra, Azinhaga de Santa Comba, Celas, 3004-548 Coimbra, Portugal.
authors.forename: Kathleen
authors.initials: K
authors.lastname: Santos
authors.affiliation: Biophysics Unit, Faculty of Medicine of University of Coimbra, Azinhaga de Santa Comba, Celas, 3004-548 Coimbra, Portugal; CIMAGO - Center of Investigation in Environment, Genetics and Oncobiology, Faculty of Medicine of University of Coimbra, Azinhaga de Santa Comba, Celas, 3004-548 Coimbra, Portugal; IBILI - Institute for Biomedical Imaging and Life Science, Faculty of Medicine of University of Coimbra, Azinhaga de Santa Comba, Celas, 3004-548 Coimbra, Portugal.
authors.forename: Mafalda
authors.initials: M
authors.lastname: Laranjo
authors.affiliation: Biophysics Unit, Faculty of Medicine of University of Coimbra, Azinhaga de Santa Comba, Celas, 3004-548 Coimbra, Portugal; CIMAGO - Center of Investigation in Environment, Genetics and Oncobiology, Faculty of Medicine of University of Coimbra, Azinhaga de Santa Comba, Celas, 3004-548 Coimbra, Portugal; IBILI - Institute for Biomedical Imaging and Life Science, Faculty of Medicine of University of Coimbra, Azinhaga de Santa Comba, Celas, 3004-548 Coimbra, Portugal.
authors.forename: Ana Margarida
authors.initials: AM
authors.lastname: Abrantes
authors.affiliation: Biophysics Unit, Faculty of Medicine of University of Coimbra, Azinhaga de Santa Comba, Celas, 3004-548 Coimbra, Portugal; IBILI - Institute for Biomedical Imaging and Life Science, Faculty of Medicine of University of Coimbra, Azinhaga de Santa Comba, Celas, 3004-548 Coimbra, Portugal.
authors.forename: Ana F
authors.initials: AF
authors.lastname: Brito
authors.affiliation: CIMAGO - Center of Investigation in Environment, Genetics and Oncobiology, Faculty of Medicine of University of Coimbra, Azinhaga de Santa Comba, Celas, 3004-548 Coimbra, Portugal; Applied Molecular Biology, University Clinic of Haematology, Faculty of Medicine of University of Coimbra, Coimbra, Portugal.
authors.forename: Cristina
authors.initials: C
authors.lastname: Gonçalves
authors.affiliation: CIMAGO - Center of Investigation in Environment, Genetics and Oncobiology, Faculty of Medicine of University of Coimbra, Azinhaga de Santa Comba, Celas, 3004-548 Coimbra, Portugal; Applied Molecular Biology, University Clinic of Haematology, Faculty of Medicine of University of Coimbra, Coimbra, Portugal.
authors.forename: Ana Bela
authors.initials: AB
authors.lastname: Sarmento Ribeiro
authors.affiliation: Biophysics Unit, Faculty of Medicine of University of Coimbra, Azinhaga de Santa Comba, Celas, 3004-548 Coimbra, Portugal; CIMAGO - Center of Investigation in Environment, Genetics and Oncobiology, Faculty of Medicine of University of Coimbra, Azinhaga de Santa Comba, Celas, 3004-548 Coimbra, Portugal; IBILI - Institute for Biomedical Imaging and Life Science, Faculty of Medicine of University of Coimbra, Azinhaga de Santa Comba, Celas, 3004-548 Coimbra, Portugal.
authors.forename: M Filomena
authors.initials: MF
authors.lastname: Botelho
authors.affiliation: Department of Chemistry, University of Coimbra, 3004-535 Coimbra, Portugal.
authors.forename: Maria I L
authors.initials: MI
authors.lastname: Soares
authors.affiliation: Department of Chemistry, University of Coimbra, 3004-535 Coimbra, Portugal.
authors.forename: Andreia S R
authors.initials: AS
authors.lastname: Oliveira
authors.affiliation: Department of Chemistry, University of Coimbra, 3004-535 Coimbra, Portugal. Electronic address: tmelo@ci.uc.pt.
authors.forename: Teresa M V D
authors.initials: TM
authors.lastname: Pinho e Melo
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000378:metabolism* / Q000473:pathology; D002453:Cell Cycle / Q000187:drug effects; D016923:Cell Death / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D005260:Female; D006801:Humans; D061986:MCF-7 Cells; D015394:Molecular Structure; D011758:Pyrroles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
chemical_list: C000594240:6,7-bis(hydroxymethyl)-1H,3H-pyrrolo(1,2-c)thiazole; D000970:Antineoplastic Agents; D011758:Pyrroles; D013844:Thiazoles
keywords: 6,7-Bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazole; Antitumor activity; Breast cancer; Triple-negative breast cancer