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Plomestane

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Plomestane
Clinical data
Other namesMDL-18962; Propargylestrenedione; PED; 10-(2-Propyn-1-yl)estr-4-ene-3,17-dione; 10-Propargylestr-4-ene-3,17-dione
ATC code
  • None
Identifiers
  • 10H-(2-Propynyl)-estr-4-ene-3,17-dione
CAS Number
PubChemCID
ChemSpider
UNII
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC21H26O2
Molar mass310.437 g·mol−1
3D model (JSmol)
  • O=C4\C=C3/[C@@](CC#C)([C@H]2CC[C@@]1(C(=O)CC[C@H]1[C@@H]2CC3)C)CC4
  • InChI=1S/C21H26O2/c1-3-10-21-12-8-15(22)13-14(21)4-5-16-17-6-7-19(23)20(17,2)11-9-18(16)21/h1,13,16-18H,4-12H2,2H3/t16-,17-,18-,20-,21-/m0/s1
  • Key:JKPDEYAOCSQBSZ-OEUJLIAZSA-N

Plomestane (INNTooltip International Nonproprietary Name,USANTooltip United States Adopted Name; former developmental code nameMDL-18962; also known aspropargylestrenedione,PED) is asteroidal,irreversiblearomatase inhibitor which was under development byMarion Merrell Dow/Hoechst Marion Russell (nowHoechst AG) as anantineoplastic agent for the treatment ofbreast cancer.[1][2][3][4][5] It was found to be effective inpreclinical studies and was also found to produce fewadverse effects in humanclinical trials, significantly reducingestrogen levels with a single administration.[5] However, development of the drug for clinical use was halted due to "technical issues" and it was never marketed.[6]

In addition to its activity as an aromatase inhibitor, plomestane has weakandrogenic properties.[5]

See also

[edit]

References

[edit]
  1. ^Macdonald F (1997).Dictionary of Pharmacological Agents. CRC Press. p. 1635.ISBN 978-0-412-46630-4. Retrieved19 May 2012.
  2. ^Morton IK, Hall JM (1999).Concise Dictionary of Pharmacological Agents: Properties and Synonyms. Springer. p. 227.ISBN 978-0-7514-0499-9. Retrieved20 May 2012.
  3. ^Lombardi P (June 1995)."The irreversible inhibition of aromatase (oestrogen synthetase) by steroidal compounds".Current Pharmaceutical Design.1. Bentham Science Publishers: 23–50 (45).doi:10.2174/1381612801666220524190226.S2CID 249298105. Retrieved20 May 2012.
  4. ^Kreider RB, Leutholtz BC, Katch FI, Katch VL (2009).Exercise and Sport Nutrition. Exercise & Sport Nutrition. p. 350.ISBN 978-0-9742965-6-2. Retrieved20 May 2012.
  5. ^abcKelloff GJ, Lubet RA, Lieberman R, et al. (January 1998)."Aromatase inhibitors as potential cancer chemopreventives".Cancer Epidemiology, Biomarkers & Prevention.7 (1):65–78.PMID 9456245.
  6. ^Avendaño C, Menéndez JC (4 June 2008).Medicinal Chemistry of Anticancer Drugs. Elsevier. p. 69.ISBN 978-0-444-52824-7. Retrieved20 May 2012.


ARTooltip Androgen receptor
Agonists
SARMsTooltip Selective androgen receptor modulator
Antagonists
GPRC6A
Agonists


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