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Your search keyword '"Methane toxicity"' showing total 2 results
Start Over Descriptor "Methane toxicity" Journal chemmedchem
2 results on '"Methane toxicity"'

1. Anticancer Gold N-Heterocyclic Carbene Complexes: A Comparative in vitro and ex vivo Study.

Author

Estrada-Ortiz N, Guarra F, de Graaf IAM, Marchetti L, de Jager MH, Groothuis GMM, Gabbiani C, and Casini A

Subjects
Animals, Antineoplastic Agents toxicity, Cell Line, Tumor, Heterocyclic Compounds toxicity, Humans, Kidney drug effects, Male, Methane analogs & derivatives, Methane chemistry, Methane pharmacology, Methane toxicity, Neoplasms drug therapy, Organogold Compounds toxicity, Rats, Wistar, Antineoplastic Agents chemistry, Antineoplastic Agents pharmacology, Heterocyclic Compounds chemistry, Heterocyclic Compounds pharmacology, Organogold Compounds chemistry, Organogold Compounds pharmacology
Abstract

A series of organometallic Au I N-heterocyclic carbene (NHC) complexes was synthesized and characterized for anticancer activity in four human cancer cell lines. The compounds' toxicity in healthy tissue was determined using precision-cut kidney slices (PCKS) as a tool to determine the potential selectivity of the gold complexes ex vivo. All evaluated compounds presented cytotoxic activity toward the cancer cells in the nano- or low micromolar range. The mixed Au I NHC complex, (tert-butylethynyl)-1,3-bis-(2,6-diisopropylphenyl)imidazol-2-ylidene gold(I), bearing an alkynyl moiety as ancillary ligand, showed high cytotoxicity in cancer cells in vitro, while being barely toxic in healthy rat kidney tissues. The obtained results open new perspectives toward the design of mixed NHC-alkynyl gold complexes for cancer therapy., (© 2017 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.)

Published
2017
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2. Synthesis of 4,4'-Diaminotriphenylmethanes with Potential Selective Estrogen Receptor Modulator (SERM)-like Activity.

Author

Guedes G, Amesty Á, Jiménez-Monzón R, Marrero-Alonso J, Díaz M, Fernández-Pérez L, and Estévez-Braun A

Subjects
Binding Sites, Cell Proliferation drug effects, Female, Humans, MCF-7 Cells, Methane chemical synthesis, Methane toxicity, Molecular Docking Simulation, Protein Binding, Protein Structure, Tertiary, Receptors, Estrogen chemistry, Receptors, Estrogen genetics, Selective Estrogen Receptor Modulators chemistry, Selective Estrogen Receptor Modulators toxicity, Transcriptional Activation drug effects, Methane chemistry, Receptors, Estrogen metabolism, Selective Estrogen Receptor Modulators chemical synthesis
Abstract

In this study, a series of new 4,4'-diaminotriphenylmethanes was efficiently synthesized from aromatic aldehydes and 2,5-dimethoxybenzenamine under microwave irradiation in the presence of Sc(OTf)3 as a catalyst. Antiproliferative activity was assessed by using the MCF-7 estrogen receptor (ER)-positive breast cancer cell line, and antagonist/agonist transcriptional activities were determined. Docking studies and competition studies of triphenylmethanes and radiolabeled estradiol determined that these compounds do not bind the ER, indicating that triphenylmethane-induced changes in proliferative and transcriptional activities differ from conventional mechanisms of action triggered by other selective ER modulators., (© 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)

Published
2015
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