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NNC 45-0095

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
NNC 45-0095
Clinical data
Other namesNNC-450095
Drug classSelective estrogen receptor modulator
Identifiers
  • 4-(1-ethylpyrrolo[2,1,5-cd]indolizin-2-yl)phenol
CAS Number
PubChemCID
ChemSpider
UNII
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC18H15NO
Molar mass261.324 g·mol−1
3D model (JSmol)
  • CCC1=C(C2=CC=C3N2C1=CC=C3)C4=CC=C(C=C4)O
  • InChI=1S/C18H15NO/c1-2-15-16-5-3-4-13-8-11-17(19(13)16)18(15)12-6-9-14(20)10-7-12/h3-11,20H,2H2,1H3
  • Key:GBHFDPQPLXKNIU-UHFFFAOYSA-N

NC 45-0095 is asyntheticnonsteroidalselective estrogen receptor modulator (SERM) which was under development byNovo Nordisk for the treatment ofpostmenopausal osteoporosis but was never marketed.[1][2][3][4][5] It is apartial agonist of theestrogen receptor (IC50Tooltip half-maximal inhibitory concentration (forbinding inhibition) = 9.5 nM;EC50Tooltip half-maximal effective concentration = 13 nM) with mixedestrogenic andantiestrogenic activity, and shows full estrogenic activity inbone anduterus (EmaxTooltip maximal efficacy (relative tomoxestrol, in Ishikawaendometrial cancercell line) = 105%).[1][4] The compound is apyrroloindolizinederivative.[1][2] Its development was discontinued by 2003.[5]

See also

[edit]

References

[edit]
  1. ^abcJørgensen AS, Jacobsen P, Christiansen LB, Bury PS, Kanstrup A, Thorpe SM, et al. (February 2000). "Synthesis and pharmacology of a novel pyrrolo[2,1,5-cd] indolizine (NNC 45-0095), a high affinity non-steroidal agonist for the estrogen receptor".Bioorganic & Medicinal Chemistry Letters.10 (4):399–402.doi:10.1016/S0960-894X(00)00015-9.PMID 10714509.
  2. ^abSharma V, Kumar V (2014). "Indolizine: a biologically active moiety".Medicinal Chemistry Research.23 (8):3593–3606.doi:10.1007/s00044-014-0940-1.ISSN 1054-2523.S2CID 2643469.
  3. ^Wallace OB, Richardson TI, Dodge JA (2003). "Estrogen receptor modulators: relationships of ligand structure, receptor affinity and functional activity".Current Topics in Medicinal Chemistry.3 (14):1663–1682.doi:10.2174/1568026033451727.PMID 14683521.
  4. ^abMeegan MJ, Lloyd DG (January 2005)."Understanding the Molecular Mechanism of Action of Estrogen Receptor Modulators. Frontiers in Medicinal Chemistry-Online". In Atta-ur-Rahman, Reitz AB (eds.).Frontiers in Medicinal Chemistry. Vol. 2. Bentham Science Publishers. pp. 183–231 (206).ISBN 978-1-60805-205-9.
  5. ^ab"NNC 450095".AdisInsight. Springer Nature Switzerland AG.
ERTooltip Estrogen receptor
Agonists
Mixed
(SERMsTooltip Selective estrogen receptor modulators)
Antagonists
GPERTooltip G protein-coupled estrogen receptor
Agonists
Antagonists
Unknown


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