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Synthesis and biological evaluation of new antioxidant and antiproliferative chalcogenobiotin derivatives for bladder carcinoma treatment

Institution:	1. LabSelen-NanoBio – Departamento de Química, Universidade Federal de Santa Maria, Santa Maria, Brazil;2. Laboratório de Bioquímica Toxicológica – Departamento de Bioquímica e Biologia Molecular, Universidade Federal de Santa Maria, Santa Maria, Brazil;3. 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 Cep 96010-900, Brazil;4. Department of Radiology, University of Illinois at Chicago, Chicago, IL, United States;5. Department of Biochemistry & Molecular Genetics, University of Illinois at Chicago, Chicago, IL, United States;6. National Center for Supercomputing Applications, University of Illinois at Urbana-Champaign, Urbana, IL, United States;1. Department of Chemistry and Biochemistry, The City College of New York, City University of New York and CUNY Institute for Macromolecular Assemblies, New York, NY 10031, USA;2. Department of Chemistry, Hunter College of CUNY, New York, NY 10065, USA;3. Ph.D. Program in Chemistry, The Graduate Center of the City University of New York (CUNY), New York, NY 10016, USA;4. Ph.D. Program in Biochemistry, The Graduate Center of the City University of New York (CUNY), New York, NY 10016, USA;1. Department of Biochemistry, Kangwon National University, Chuncheon 24341, Republic of Korea;2. Proteogen Inc., Seoul, Republic of Korea;3. Shebah Biotech Inc., G-Tech Village, Chuncheon, Republic of Korea;1. Department of Biomedical & Pharmaceutical Sciences, University of Montana, Missoula, MT 59812, United States;2. Skaggs School of Pharmacy and Pharmaceutical Sciences, Anschutz Medical Campus, University of Colorado, Aurora, CO 80045, United States;3. Department of Chemistry, Ithaca College, 953 Danby Road, Ithaca, NY 14850, United States;5. Department of Chemistry and Biochemistry, University of Montana, Missoula, MT 59812, United States;1. Department of Medicinal Chemistry, Xiangya School of Pharmaceutical Sciences, Central South University, Changsha 410013, China;2. Department of Dermatology, Xiangya Hospital, Central South University, Changsha 410008, China;1. Department of Biosciences, Jamia Millia Islamia, Jamia Nagar, New Delhi 110025, India;2. Centre for Interdisciplinary Research in Basic Sciences, Jamia Millia Islamia, Jamia Nagar, New Delhi 110025, India;3. Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, New Delhi 110025, India;4. Department of Pharmacognosy, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia;5. Organisch-Chemisches Institut, Westfälische Wilhelms-Universität Münster, 48149, Germany

Abstract:	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.

Keywords:	Antioxidants Antiproliferative activity Biological activity Biotin Chalcogen-vitamins DPPH"} {"#name":"keyword" "$":{"id":"k0035"} "$$":[{"#name":"text" "_":"2 2-diphenyl-1-picrylhydrazyl DBU"} {"#name":"keyword" "$":{"id":"k0045"} "$$":[{"#name":"text" "_":"1 8-diazabicyclo(5 4 0)undec-7-ene MTT"} {"#name":"keyword" "$":{"id":"k0055"} "$$":[{"#name":"text" "_":"3-(4 5-dimethylthiazol-2-yl)-2 5-diphenyltetrazolium bromide) TBARS"} {"#name":"keyword" "$":{"id":"k0065"} "$$":[{"#name":"text" "_":"thiobarbituric acid reactive substances BHT"} {"#name":"keyword" "$":{"id":"k0075"} "$$":[{"#name":"text" "_":"2 6-bis(1 1-dimethylethyl)-4-methylphenol AST"} {"#name":"keyword" "$":{"id":"k0085"} "$$":[{"#name":"text" "_":"aspartate aminotransferase ALT"} {"#name":"keyword" "$":{"id":"k0095"} "$$":[{"#name":"text" "_":"alanine aminotransferase
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