C-6α- vs C-7α-Substituted Steroidal Aromatase Inhibitors: Which Is Better? Synthesis, Biochemical Evaluation, Docking Studies, and Structure-Activity Relationships.

Aromatase Inhibitors / chemistry Humans Molecular Docking Simulation Steroids / chemistry Structure-Activity Relationship

Journal

Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531

Informations de publication

Date de publication:
11 04 2019
Historique:
pubmed: 12 3 2019
medline: 15 9 2020
entrez: 12 3 2019
Statut: ppublish

Résumé

C-6α and C-7α androstanes were studied to disclose which position among them is more convenient to functionalize to reach superior aromatase inhibition. In the first series, the study of C-6 versus C-7 methyl derivatives led to the very active compound 9 with IC

Identifiants

DOI: 10.1021/acs.jmedchem.9b00157 PMID: 30852901
pubmed: 30852901
doi: 10.1021/acs.jmedchem.9b00157
doi:

Substances chimiques

Aromatase Inhibitors 0
Steroids 0

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

3636-3657

Auteurs

Fernanda M F Roleira (FMF)

Laboratory of Pharmaceutical Chemistry, Faculty of Pharmacy , University of Coimbra , 3000-548 Coimbra , Portugal.
CIEPQPF Centre for Chemical Processes Engineering and Forest Products , University of Coimbra , 3030-790 Coimbra , Portugal.
ORCID: 0000-0003-4229-5882

Carla Varela (C)

Laboratory of Pharmaceutical Chemistry, Faculty of Pharmacy , University of Coimbra , 3000-548 Coimbra , Portugal.
CIEPQPF Centre for Chemical Processes Engineering and Forest Products , University of Coimbra , 3030-790 Coimbra , Portugal.

Cristina Amaral (C)

UCIBIO.REQUIMTE, Laboratory of Biochemistry, Department of Biological Sciences, Faculty of Pharmacy , University of Porto , 4050-313 Porto , Portugal.

Saul C Costa (SC)

Laboratory of Pharmaceutical Chemistry, Faculty of Pharmacy , University of Coimbra , 3000-548 Coimbra , Portugal.

Georgina Correia-da-Silva (G)

UCIBIO.REQUIMTE, Laboratory of Biochemistry, Department of Biological Sciences, Faculty of Pharmacy , University of Porto , 4050-313 Porto , Portugal.

Federica Moraca (F)

Laboratorio di Chimica Farmaceutica, Dipartimento di Scienze della Salute , Università Magna Græcia di Catanzaro , 88100 Catanzaro , Italy.
Department of Pharmacy , University of Naples "Federico II" , via D. Montesano 49 , 80131 , Naples , Italy.
Net4Science Academic Spin-Off , "Magna Græcia" University of Catanzaro , "S. Venuta", Catanzaro , Italy.

Giosuè Costa (G)

Laboratorio di Chimica Farmaceutica, Dipartimento di Scienze della Salute , Università Magna Græcia di Catanzaro , 88100 Catanzaro , Italy.
Net4Science Academic Spin-Off , "Magna Græcia" University of Catanzaro , "S. Venuta", Catanzaro , Italy.
ORCID: 0000-0003-0947-9479

Stefano Alcaro (S)

Laboratorio di Chimica Farmaceutica, Dipartimento di Scienze della Salute , Università Magna Græcia di Catanzaro , 88100 Catanzaro , Italy.
Net4Science Academic Spin-Off , "Magna Græcia" University of Catanzaro , "S. Venuta", Catanzaro , Italy.

Natércia A A Teixeira (NAA)

UCIBIO.REQUIMTE, Laboratory of Biochemistry, Department of Biological Sciences, Faculty of Pharmacy , University of Porto , 4050-313 Porto , Portugal.

Elisiário J Tavares da Silva (EJ)

Laboratory of Pharmaceutical Chemistry, Faculty of Pharmacy , University of Coimbra , 3000-548 Coimbra , Portugal.
CIEPQPF Centre for Chemical Processes Engineering and Forest Products , University of Coimbra , 3030-790 Coimbra , Portugal.
ORCID: 0000-0002-0390-3403

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Classifications MeSH

questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Effets physiologiques des médicaments › Hormones, substituts d'hormones et antagonistes d'hormones › Antihormones › Inhibiteurs de la synthèse des stéroïdes › Inhibiteurs de l'aromatase › C-6α- vs C-7α-Substituted Steroidal Aromatase...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › C-6α- vs C-7α-Substituted Steroidal Aromatase...
questionsmedicales.fr › Sciences de l'information › Méthodologies informatiques › Simulation numérique › Simulation de docking moléculaire › C-6α- vs C-7α-Substituted Steroidal Aromatase...
questionsmedicales.fr › Composés polycycliques › Composés à cycles fusionnés › Stéroïdes › C-6α- vs C-7α-Substituted Steroidal Aromatase...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › C-6α- vs C-7α-Substituted Steroidal Aromatase...