Modeling, Synthesis, and Biological Evaluation of Potential Retinoid-X-Receptor (RXR) Selective Agonists: Analogs of 4-[1-(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahyro-2-naphthyl)ethynyl]benzoic Acid (Bexarotene) and 6-(Ethyl(4-isobutoxy-3-isopropylphenyl)amino)nicotinic Acid (NEt-4IB).
Animals
Antineoplastic Agents
/ chemical synthesis
Apolipoproteins E
/ genetics
Bexarotene
/ analogs & derivatives
Cell Line, Tumor
Dose-Response Relationship, Drug
Gene Expression
Humans
Leukocytes
/ drug effects
Nicotinic Acids
/ chemical synthesis
Retinoid X Receptor alpha
/ agonists
Structure-Activity Relationship
leukemia
retinoid
retinoid-X-receptor
rexinoid
small molecule therapeutic
structure–activity relationship
Journal
International journal of molecular sciences
ISSN: 1422-0067
Titre abrégé: Int J Mol Sci
Pays: Switzerland
ID NLM: 101092791
Informations de publication
Date de publication:
16 Nov 2021
16 Nov 2021
Historique:
received:
27
09
2021
revised:
08
11
2021
accepted:
12
11
2021
entrez:
27
11
2021
pubmed:
28
11
2021
medline:
17
12
2021
Statut:
epublish
Résumé
Five novel analogs of 6-(ethyl)(4-isobutoxy-3-isopropylphenyl)amino)nicotinic acid-or NEt-4IB-in addition to seven novel analogs of 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic acid (bexarotene) were prepared and evaluated for selective retinoid-X-receptor (RXR) agonism alongside bexarotene (
Identifiants
pubmed: 34830251
pii: ijms222212371
doi: 10.3390/ijms222212371
pmc: PMC8624485
pii:
doi:
Substances chimiques
Antineoplastic Agents
0
ApoE protein, human
0
Apolipoproteins E
0
Nicotinic Acids
0
RXRA protein, human
0
Retinoid X Receptor alpha
0
Bexarotene
A61RXM4375
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Subventions
Organisme : NCI NIH HHS
ID : R15 CA249617
Pays : United States
Organisme : NCI NIH HHS
ID : R15 CA139364
Pays : United States
Organisme : NCI NIH HHS
ID : P30 CA091842
Pays : United States
Organisme : NIH HHS
ID : R01 HL128447
Pays : United States
Organisme : NIH HHS
ID : 1 R15 CA139364-01A2
Pays : United States
Organisme : NIH HHS
ID : 1R15CA249617-01
Pays : United States
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