دورية أكاديمية
أعرض في EDS

7-Chloroquinoline-1,2,3-triazoyl carboxamides induce cell cycle arrest and apoptosis in human bladder carcinoma cells.

التفاصيل البيبلوغرافية
العنوان: 7-Chloroquinoline-1,2,3-triazoyl carboxamides induce cell cycle arrest and apoptosis in human bladder carcinoma cells.
المؤلفون: Sonego MS; Laboratório de Biotecnologia do Câncer, Programa de Pós-Graduação em Biotecnologia (PPGB), Centro de Desenvolvimento Tecnológico (CDTec), Universidade Federal de Pelotas, Campus Universitário s/n, Capão do Leão, RS, 96010-900, Brazil., Segatto NV; Laboratório de Biotecnologia do Câncer, Programa de Pós-Graduação em Biotecnologia (PPGB), Centro de Desenvolvimento Tecnológico (CDTec), Universidade Federal de Pelotas, Campus Universitário s/n, Capão do Leão, RS, 96010-900, Brazil., Damé L; Laboratório de Biotecnologia do Câncer, Programa de Pós-Graduação em Biotecnologia (PPGB), Centro de Desenvolvimento Tecnológico (CDTec), Universidade Federal de Pelotas, Campus Universitário s/n, Capão do Leão, RS, 96010-900, Brazil., Fronza M; Grupo de Pesquisa em Neurobiotecnologia (GPN), Centro de Desenvolvimento Tecnológico (CDTec), Universidade Federal de Pelotas, Pelotas, RS, 96010-900, Brazil., Gomes CB; Laboratório de Síntese Orgânica Limpa (LASOL), CCQFA, Universidade Federal de Pelotas, Campus Universitário s/n, Capão do Leão, RS, 96010-900, Brazil., Oliveira TL; Laboratório de Biotecnologia do Câncer, Programa de Pós-Graduação em Biotecnologia (PPGB), Centro de Desenvolvimento Tecnológico (CDTec), Universidade Federal de Pelotas, Campus Universitário s/n, Capão do Leão, RS, 96010-900, Brazil., Seixas FK; Laboratório de Biotecnologia do Câncer, Programa de Pós-Graduação em Biotecnologia (PPGB), Centro de Desenvolvimento Tecnológico (CDTec), Universidade Federal de Pelotas, Campus Universitário s/n, Capão do Leão, RS, 96010-900, Brazil., Savegnago L; Grupo de Pesquisa em Neurobiotecnologia (GPN), Centro de Desenvolvimento Tecnológico (CDTec), Universidade Federal de Pelotas, Pelotas, RS, 96010-900, Brazil., Schachtschneider KM; Department of Radiology, University of Illinois at Chicago, Chicago, IL, USA.; Department of Biochemistry & Molecular Genetics, University of Illinois at Chicago, Chicago, IL, USA.; National Center for Supercomputing Applications, University of Illinois at Urbana-Champaign, Urbana, IL, USA., Alves D; Laboratório de Síntese Orgânica Limpa (LASOL), CCQFA, Universidade Federal de Pelotas, Campus Universitário s/n, Capão do Leão, RS, 96010-900, Brazil., Collares T; Laboratório de Biotecnologia do Câncer, Programa de Pós-Graduação em Biotecnologia (PPGB), Centro de Desenvolvimento Tecnológico (CDTec), Universidade Federal de Pelotas, Campus Universitário s/n, Capão do Leão, RS, 96010-900, Brazil. tiago.collares@ufpel.edu.br.
المصدر: Investigational new drugs [Invest New Drugs] 2020 Aug; Vol. 38 (4), pp. 1020-1030. Date of Electronic Publication: 2019 Nov 06.
نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't
اللغة: English
بيانات الدورية: Publisher: Springer Country of Publication: United States NLM ID: 8309330 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1573-0646 (Electronic) Linking ISSN: 01676997 NLM ISO Abbreviation: Invest New Drugs Subsets: MEDLINE
أسماء مطبوعة: Publication: New York : Springer
Original Publication: Boston : M. Nijhoff, 1983-
مواضيع طبية MeSH: Amides/*pharmacology , Quinolines/*pharmacology , Triazoles/*pharmacology , Urinary Bladder Neoplasms/*drug therapy, Apoptosis/drug effects ; Cell Cycle Checkpoints/drug effects ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Cell Survival/drug effects ; Humans ; Molecular Docking Simulation ; Proto-Oncogene Proteins c-bcl-2/metabolism ; Urinary Bladder Neoplasms/metabolism
مستخلص: In the present study, the antitumoral properties of a series of 7-chloroquinoline-1,2,3-triazoyl-carboxamides (QTCA) were investigated by analyzing their cytotoxic activities against human bladder cells (5637; grade II carcinoma). In addition, their effects on cell viability, cell cycle arrest mechanisms, apoptosis induction, in silico molecular docking, and detection of pro-apoptotic and anti-apoptotic proteins were evaluated. The cytotoxicity assay identified major dose- and time-dependent cytotoxic effects in 5637 cells after they were exposed to treatment with QTCA, only minimal effects were observed on normal cells. A live/dead assay confirmed that significant cell death, arrest in the G0/G1 phase and apoptosis were associated with treatment by 1-(7-Chloroquinolin-4-yl)-5-methyl-N-phenyl-1H-1,2,3-triazole-4-carboxamide (QTCA-1) and 1-(7-Chloroquinolin-4-yl)-N-(4-fluorophenyl)-5-methyl-1H-1,2,3-triazole-4-carboxamide (QTCA-4). The in silico results indicated that these compounds acted through different mechanisms for the induction of cell cycle arrest and apoptosis. Western blotting confirmed the binding of the QTCAs to pro- and anti-apoptotic proteins. In conclusion, QTCA-1 and QTCA-4 are promising candidates for inducing cytotoxicity, cell cycle arrest, and apoptosis in human bladder cancer cells.
فهرسة مساهمة: Keywords: Anticancer; Apoptosis; Bladder cancer cytotoxicity; Cell cycle arrest; Quinoline derivatives
المشرفين على المادة: 0 (Amides)
0 (BCL2 protein, human)
0 (Proto-Oncogene Proteins c-bcl-2)
0 (Quinolines)
0 (Triazoles)
تواريخ الأحداث: Date Created: 20191108 Date Completed: 20210909 Latest Revision: 20210909
رمز التحديث: 20221213
DOI: 10.1007/s10637-019-00861-w
PMID: 31696365
قاعدة البيانات: MEDLINE
الوصف
تدمد:1573-0646
DOI:10.1007/s10637-019-00861-w