Click estradiol dimers with novel aromatic bridging units: synthesis and anticancer evaluation.

Humans Antineoplastic Agents / pharmacology Drug Screening Assays, Antitumor Estradiol / pharmacology Molecular Structure Structure-Activity Relationship Cell Proliferation / drug effects Dose-Response Relationship, Drug Dimerization Click Chemistry Cell Line, Tumor
Estradiol cancer cell dimer in silico tubulin

Journal

Journal of enzyme inhibition and medicinal chemistry
ISSN: 1475-6374
Titre abrégé: J Enzyme Inhib Med Chem
Pays: England
ID NLM: 101150203

Informations de publication

Date de publication:
Dec 2024
Historique:
medline: 21 6 2024
pubmed: 21 6 2024
entrez: 21 6 2024
Statut: ppublish

Résumé

Estradiol dimers (EDs) possess significant anticancer activity by targeting tubulin dynamics. In this study, we synthesised 12 EDs variants via copper-catalysed azide-alkyne cycloaddition (CuAAC) reaction, focusing on structural modifications within the aromatic bridge connecting two estradiol moieties.

Identifiants

DOI: 10.1080/14756366.2024.2367139 PMID: 38904149
pubmed: 38904149
doi: 10.1080/14756366.2024.2367139
doi:

Substances chimiques

Antineoplastic Agents 0
Estradiol 4TI98Z838E

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

2367139

Auteurs

Jiří Řehulka (J)

Institute of Molecular and Translational Medicine, Faculty of Medicine and Dentistry, Palacký University, Olomouc, Czech Republic.

Michal Jurášek (M)

Department of Chemistry of Natural Compounds, University of Chemistry and Technology Prague, Praha 6, Czech Republic.

Pavel Dráber (P)

Department of Biology of Cytoskeleton, Institute of Molecular Genetics of the Czech Academy of Sciences, Praha 4, Czech Republic.

Aleksandra Ivanová (A)

Institute of Molecular and Translational Medicine, Faculty of Medicine and Dentistry, Palacký University, Olomouc, Czech Republic.

Soňa Gurská (S)

Institute of Molecular and Translational Medicine, Faculty of Medicine and Dentistry, Palacký University, Olomouc, Czech Republic.

Kateřina Ječmeňová (K)

Institute of Molecular and Translational Medicine, Faculty of Medicine and Dentistry, Palacký University, Olomouc, Czech Republic.

Olena Mokshyna (O)

Institute of Molecular and Translational Medicine, Faculty of Medicine and Dentistry, Palacký University, Olomouc, Czech Republic.
Institute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences, Praha 6, Czech Republic.

Marián Hajdúch (M)

Institute of Molecular and Translational Medicine, Faculty of Medicine and Dentistry, Palacký University, Olomouc, Czech Republic.
Laboratory of Experimental Medicine, Institute of Molecular and Translational Medicine, University Hospital Olomouc, Olomouc, Czech Republic.

Pavel Polishchuk (P)

Institute of Molecular and Translational Medicine, Faculty of Medicine and Dentistry, Palacký University, Olomouc, Czech Republic.

Pavel B Drašar (PB)

Department of Chemistry of Natural Compounds, University of Chemistry and Technology Prague, Praha 6, Czech Republic.

Petr Džubák (P)

Institute of Molecular and Translational Medicine, Faculty of Medicine and Dentistry, Palacký University, Olomouc, Czech Republic.
Laboratory of Experimental Medicine, Institute of Molecular and Translational Medicine, University Hospital Olomouc, Olomouc, Czech Republic.

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Click estradiol dimers with novel aromatic...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Antinéoplasiques › Click estradiol dimers with novel aromatic...
questionsmedicales.fr › Techniques d'investigation › Évaluation préclinique de médicament › Tests de criblage d'agents antitumoraux › Click estradiol dimers with novel aromatic...
questionsmedicales.fr › Hormones gonadiques › Hormones sexuelles stéroïdiennes › Congénères de l'oestradiol › Oestradiol › Click estradiol dimers with novel aromatic...
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › Click estradiol dimers with novel aromatic...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Click estradiol dimers with novel aromatic...
questionsmedicales.fr › Phénomènes physiologiques › Croissance et développement › Croissance › Processus de croissance cellulaire › Prolifération cellulaire › Click estradiol dimers with novel aromatic...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes toxicologiques › Relation dose-effet des médicaments › Click estradiol dimers with novel aromatic...
questionsmedicales.fr › Métabolisme › Dimérisation › Click estradiol dimers with novel aromatic...
questionsmedicales.fr › Technologie, industrie et agriculture › Technologie › Technologie pharmaceutique › Techniques de chimie synthétique › Chimie click › Click estradiol dimers with novel aromatic...
questionsmedicales.fr › Cellules › Cellules cultivées › Cellules cancéreuses en culture › Lignée cellulaire tumorale › Click estradiol dimers with novel aromatic...