Synthesis, antiproliferative and mitochondrial impairment activities of bis-alkyl-amino transplatinum complexes

Autor:	Lisa Dalla Via, Silvia Grancara, Antonio Toninello, Arianna Adami, Simona Samaritani, Luca Labella, Daniela Belli Dell'Amico, Pamela Martinis, Aída Nelly García-Argáez
Rok vydání:	2013
Předmět:	Phosphines Stereochemistry Clinical Biochemistry Pharmaceutical Science Antineoplastic Agents Apoptosis Antiproliferative activity Mitochondrion medicine.disease_cause Membrane Potential Biochemistry Cell Line Isomerism Coordination Complexes Cell Line Tumor Drug Discovery medicine Humans Transplatinum complexes Molecular Biology Cell Proliferation Platinum Membrane Potential Mitochondrial Mitochondrial permeability transition Tumor Cell growth Chemistry Drug Discovery3003 Pharmaceutical Science Organic Chemistry Mitochondria Oxidative stress Mitochondrial HeLa Cells 3003 Molecular Medicine Membrane Mechanism of action Mitochondrial permeability transition pore Cell culture medicine.symptom
Zdroj:	Bioorganic & Medicinal Chemistry. 21:6965-6972
ISSN:	0968-0896
Popis:	A convenient synthetic route and the characterization of complexes trans-[PtCl2(L)(PPh3)] (L=Et2NH (2), (PhCH2)2NH (3), (HOCH2CH2)2NH) (4) are reported. The antiproliferative activity was evaluated on three human tumor cell lines. The investigation on the mechanism of action highlighted for the most active complex 4 the capacity to affect mitochondrial functions. In particular, both the induction of the mitochondrial permeability transition phenomenon and an aspecific membrane damage occurred, depending on concentration.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0dc0b4f675b6029ed0d21617e9662a8b https://doi.org/10.1016/j.bmc.2013.09.025 Zobrazit plný text záznamu Full Text from ScienceDirect