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Nonsteroidal antiandrogen of the quinoline group
LG-120907
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Other names | 1,2,3,4-Tetrahydro-2,2-dimethyl-6-trifluoromethyl-8-pyridono[5,6-g]quinoline |
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Drug class |
Nonsteroidal antiandrogen |
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2,2-Dimethyl-6-(trifluoromethyl)-1,9-dihydropyrido[3,2-g]quinolin-8-one
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CAS Number | |
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PubChem
CID | |
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ChemSpider | |
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ChEMBL | |
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Formula | C15H13F3N2O |
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Molar mass | 294.277 g·mol−1 |
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3D model (
JSmol) | |
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CC1(C=CC2=C(N1)C=C3C(=C2)C(=CC(=O)N3)C(F)(F)F)C
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InChI=1S/C15H13F3N2O/c1-14(2)4-3-8-5-9-10(15(16,17)18)6-13(21)19-12(9)7-11(8)20-14/h3-7,20H,1-2H3,(H,19,21) Key:MMLSXRYBGYGQEP-UHFFFAOYSA-N
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LG-120907 is a
nonsteroidal antiandrogen (NSAA) of the
quinoline group which was developed by
Ligand Pharmaceuticals along with
selective androgen receptor modulators (SARMs) like
LG-121071 and was never marketed.
[1]
[2]
[3]
[4] The drug is a high-
affinity
antagonist of the
androgen receptor (AR) with a Ki value of 26 nM and has been found to inhibit
growth of the
ventral prostate and
seminal vesicles in male rats without increasing circulating levels of
luteinizing hormone or
testosterone.
[1]
[2]
[3] However, this
tissue selectivity has not been assessed in humans.
[5] LG-120907 is
orally active and shows greater oral
potency than the
aryl
propionamide NSAA
flutamide.
[1]
[3]
[4]
The 7-
fluoro
derivative of LG-120907,
LG-105, is also a potent NSAA, and appears to possess greater potency in comparison.
[3] Conversely, the 6-
ethyl, 8-di
desmethyl
analogue of LG-120907, LG-121071, is a SARM with potent
androgenic activity equivalent to that of
dihydrotestosterone (DHT).
[1]
[3]
References
- ^
a
b
c
d Chengalvala M, Oh T, Roy AK (2005). "Selective androgen receptor modulators". Expert Opinion on Therapeutic Patents. 13 (1): 59–66.
doi:
10.1517/13543776.13.1.59.
ISSN
1354-3776.
S2CID
219188263.
- ^
a
b Mohler ML, Nair VA, Hwang DJ, Rakov IM, Patil R, Miller DD (2005). "Nonsteroidal tissue selective androgen receptor modulators: a promising class of clinical candidates". Expert Opinion on Therapeutic Patents. 15 (11): 1565–1585.
doi:
10.1517/13543776.15.11.1565.
ISSN
1354-3776.
S2CID
96279138.
- ^
a
b
c
d
e Gao W, Kim J, Dalton JT (August 2006).
"Pharmacokinetics and pharmacodynamics of nonsteroidal androgen receptor ligands". Pharmaceutical Research. 23 (8): 1641–1658.
doi:
10.1007/s11095-006-9024-3.
PMC
2072875.
PMID
16841196.
- ^
a
b Nyrönen TH, Söderholm AA (January 2010). "Structural basis for computational screening of non-steroidal androgen receptor ligands". Expert Opinion on Drug Discovery. 5 (1): 5–20.
doi:
10.1517/17460440903468680.
PMID
22823968.
S2CID
21630468.
-
^ Hoffmann J, Sommer A (30 January 2007).
"Anti-hormone therapy: principles of endocrine therapy of cancer.". In Bradbury R (ed.). Cancer. Springer Science & Business Media. pp. 19-82 (67).
ISBN
978-3-540-33120-9.
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ARTooltip Androgen receptor | Agonists | |
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SARMsTooltip Selective androgen receptor modulator | |
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Antagonists | |
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GPRC6A | |
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