NNC 45-0095

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
PubChem CID
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 a synthetic nonsteroidal selective estrogen receptor modulator (SERM) which was under development by Novo Nordisk for the treatment of postmenopausal osteoporosis but was never marketed.[1][2][3][4][5] It is a partial agonist of the estrogen receptor (IC50Tooltip half-maximal inhibitory concentration (for binding inhibition) = 9.5 nM; EC50Tooltip half-maximal effective concentration = 13 nM) with mixed estrogenic and antiestrogenic activity, and shows full estrogenic activity in bone and uterus (EmaxTooltip maximal efficacy (relative to moxestrol, in Ishikawa endometrial cancer cell line) = 105%).[1][4] The compound is a pyrroloindolizine derivative.[1][2] Its development was discontinued by 2003.[5]

See also

References

  1. ^ a b c Jørgensen 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. ^ a b Sharma 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. ^ a b Meegan 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. ^ a b "NNC 450095". AdisInsight. Springer Nature Switzerland AG.


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