دورية أكاديمية
A Novel Triazole Derivative Drug Presenting In Vitro and In Vivo Anticancer Properties.
| العنوان: | A Novel Triazole Derivative Drug Presenting In Vitro and In Vivo Anticancer Properties. |
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| المؤلفون: | Filho RI; Laboratorio de Oncobiologia Molecular (LabOMol), Departamento de Biotecnologia Farmaceutica, Faculdade de Farmacia, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, 21941-902, Brazil., Gonzaga DTG; Instituto de Quimica, Campus do Valonguinho, Universidade Federal Fluminense, Niteroi-RJ, 24020-141, Brazil., Demaria TM; Laboratorio de Enzimologia e Controle do Metabolismo (LabECoM), Departamento de Biotecnologia Farmaceutica, Faculdade de Farmacia, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, 21941-902, Brazil., Leandro JGB; Laboratorio de Enzimologia e Controle do Metabolismo (LabECoM), Departamento de Biotecnologia Farmaceutica, Faculdade de Farmacia, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, 21941-902, Brazil., Costa DCS; Instituto de Quimica, Campus do Valonguinho, Universidade Federal Fluminense, Niteroi-RJ, 24020-141, Brazil., Ferreira VF; Instituto de Quimica, Campus do Valonguinho, Universidade Federal Fluminense, Niteroi-RJ, 24020-141, Brazil., Sola-Penna M; Laboratorio de Enzimologia e Controle do Metabolismo (LabECoM), Departamento de Biotecnologia Farmaceutica, Faculdade de Farmacia, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, 21941-902, Brazil., de C da Silva F; Instituto de Quimica, Campus do Valonguinho, Universidade Federal Fluminense, Niteroi-RJ, 24020-141, Brazil., Zancan P; Laboratorio de Oncobiologia Molecular (LabOMol), Departamento de Biotecnologia Farmaceutica, Faculdade de Farmacia, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, 21941-902, Brazil. |
| المصدر: | Current topics in medicinal chemistry [Curr Top Med Chem] 2018; Vol. 18 (17), pp. 1483-1493. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Bentham Science Publishers Country of Publication: United Arab Emirates NLM ID: 101119673 Publication Model: Print Cited Medium: Internet ISSN: 1873-4294 (Electronic) Linking ISSN: 15680266 NLM ISO Abbreviation: Curr Top Med Chem Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: Saif Zone, Sharjah, U.A.E. : Bentham Science Publishers Original Publication: Hilversum, The Netherlands : Bentham Science Publishers, c2001- |
| مواضيع طبية MeSH: | Antineoplastic Agents, Phytogenic/*pharmacology , Triazoles/*pharmacology, Animals ; Antineoplastic Agents, Phytogenic/chemistry ; Apoptosis/drug effects ; Cell Cycle/drug effects ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Cell Survival/drug effects ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Female ; Humans ; Membrane Potential, Mitochondrial/drug effects ; Mice ; Mice, Inbred C57BL ; Molecular Structure ; Reactive Oxygen Species/metabolism ; Structure-Activity Relationship ; Triazoles/chemistry |
| مستخلص: | Background: Cancer is a major cause of death worldwide, despite many different drugs available to treat the disease. This high mortality rate is largely due to the complexity of the disease, which results from several genetic and epigenetic changes. Therefore, researchers are constantly searching for novel drugs that can target different and multiple aspects of cancer. Experimental: After a screening, we selected one novel molecule, out of ninety-four triazole derivatives, that strongly affects the viability and proliferation of the human breast cancer cell line MCF-7, with minimal effects on non-cancer cells. The drug, named DAN94, induced a dose-dependent decrease in MCF-7 cells viability, with an IC50 of 3.2 ± 0.2 µM. Additionally, DAN94 interfered with mitochondria metabolism promoting reactive oxygen species production, triggering apoptosis and arresting the cancer cells on G1/G0 phase of cell cycle, inhibiting cell proliferation. These effects are not observed when the drug was tested in the non-cancer cell line MCF10A. Using a mouse model with xenograft tumor implants, the drug preventing tumor growth presented no toxicity for the animal and without altering biochemical markers of hepatic function. Results and Conclusion: The novel drug DAN94 is selective for cancer cells, targeting the mitochondrial metabolism, which culminates in the cancer cell death. In the end, DAN94 has been shown to be a promising drug for controlling breast cancer with minimal undesirable effects. (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.) |
| فهرسة مساهمة: | Keywords: Apoptosis; Cancer; Cell cycle; Novel triazole; Reactive oxygen species; Viability. |
| المشرفين على المادة: | 0 (Antineoplastic Agents, Phytogenic) 0 (Reactive Oxygen Species) 0 (Triazoles) |
| تواريخ الأحداث: | Date Created: 20180918 Date Completed: 20190114 Latest Revision: 20190114 |
| رمز التحديث: | 20240829 |
| DOI: | 10.2174/1568026618666180917100640 |
| PMID: | 30221602 |
| قاعدة البيانات: | MEDLINE |
| تدمد: | 1873-4294 |
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| DOI: | 10.2174/1568026618666180917100640 |