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Volumn 18, Issue 15, 2008, Pages 4339-4343

Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064

Author keywords

Bile acid receptor; Farnesoid X receptor agonist; FXR; FXR X ray co crystal structure; GSK8062; GW 4064; Naphthoic acid; NR1H4; Nuclear receptor modulator

Indexed keywords

3 [2 [2 CHLORO 4 [3 (2,6 DICHLOROPHENYL) 5 ISOPROPYL 4 ISOXAZOLYLMETHOXY]PHENYL]VINYL]BENZOIC ACID; FARNESOID X RECEPTOR AGONIST; GSK 8062; HORMONE RECEPTOR STIMULATING AGENT; UNCLASSIFIED DRUG;

EID: 47749128054     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.06.073     Document Type: Article
Times cited : (123)

References (41)
  • 33
    • 47749109913 scopus 로고    scopus 로고
    • Deaton, D. N.; McFadyen, R. B.; Navas, F., III; Caldwell, R.; Spearing, P. K. PCT Int. Appl. WO 076260, 2007.
    • Deaton, D. N.; McFadyen, R. B.; Navas, F., III; Caldwell, R.; Spearing, P. K. PCT Int. Appl. WO 076260, 2007.
  • 35
    • 47749100111 scopus 로고    scopus 로고
    • Morand, E. F.; Iskander, M.N. PCT Int. Appl. WO 104178, 2003
    • Morand, E. F.; Iskander, M.N. PCT Int. Appl. WO 104178, 2003
  • 37
    • 47749100887 scopus 로고    scopus 로고
    • note
    • Although methyl 7-hydroxy-2-naphthoate 3c is known in the literature, it was prepared from commercially available 7-methoxy-2-naphthol in three synthetic steps. First, 7-methoxy-2-naphthol was converted into the triflate with trifluoromethanesulfonic anhydride. Then, palladium-mediated carbonylation of the triflate under a carbon monoxide atmosphere in methanol and N,N-dimethylformamide provided methyl 7-methoxy-2-naphthoate. Finally, cleavage of the methyl ether with boron tribromide gave the desired methyl 7-hydroxy-2-naphthoate 3c.
  • 40
    • 47749086706 scopus 로고    scopus 로고
    • note
    • 741-761SRC-1, K-E-S-K-D-H-Q-L-L-R-Y-L-L-D-K-D-E-K-D-L-R) derived from steroid receptor coactivator-1 (SRC-1) was added to 1.5 mol protein equivalents and incubated on ice for another hour. The protein complexes were concentrated to 12 mg/ml or higher and crystallized by hanging drop vapor diffusion around the conditions 0.1 M Bis(2-hydroxyethyl)-imino-tris(hydroxymethyl)-methane, pH 6.5, 0.2 M lithium sulfate, and 20% polyethylene glycol 4000. The crystals were frozen by stepwise exchange into the same buffer, with 30% glycerol, followed by plunging into liquid nitrogen.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.