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Bioorg Med Chem ; 28(9): 115423, 2020 05 01.
Article En | MEDLINE | ID: mdl-32205047

Approximately 90% of bladder carcinomas are of the urothelial carcinoma type, which are characterized by high rates of recurrence and predisposition to progress to invasive tumors, representing one of the most costly neoplasms for health systems. Intravesical chemotherapy is a standard for the treatment of non-invasive bladder cancer. However, chemotherapy is usually aggressive and cytotoxic, which increases the death rates caused by cancer. Heterocyclic compounds which exhibit favorable pharmacokinetic and pharmacodynamic properties may enhance drug affinity for a target protein by targeting the treatment. Thus, this work presents the synthesis, characterization, and in vitro biological evaluation of new antioxidant (inhibition of lipid peroxidation, scavenging of free radical DPPH, and thiol peroxidase-like activity) and antiproliferative chalcogenobiotin derivatives and tests them against bladder carcinoma 5637 cells. A prominent response was obtained for the selected compounds, with tellurium biotin derivatives displaying effective antioxidant and antiproliferative activity. The effective compounds also demonstrated no toxicity in in vitro or in vivo studies.


Antineoplastic Agents/pharmacology , Antioxidants/pharmacology , Chalcogens/pharmacology , Urinary Bladder Neoplasms/drug therapy , Urinary Bladder/drug effects , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Antioxidants/chemical synthesis , Antioxidants/chemistry , Biphenyl Compounds/antagonists & inhibitors , Cell Line, Tumor , Cell Proliferation/drug effects , Chalcogens/chemical synthesis , Chalcogens/chemistry , Dose-Response Relationship, Drug , Drug Screening Assays, Antitumor , Humans , Lipid Peroxidation/drug effects , Molecular Structure , Picrates/antagonists & inhibitors , Structure-Activity Relationship , Urinary Bladder/pathology , Urinary Bladder Neoplasms/pathology
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