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Bioorganic and Medicinal Chemistry Letters

Volumn 11, Issue 10, 2001, Pages 1257-1260

Diaryl ether inhibitors of farnesyl-protein transferase

(13) MacTough, Suzanne C a Desolms, S Jane a Shaw, Anthony W a Abrams, Marc T a Ciccarone, Terrence M a Davide, Joseph P a Hamilton, Kelly A a Hutchinson, John H a Koblan, Kenneth S a Kohl, Nancy E a Lobell, Robert B a Robinson, Ronald G a Graham, Samuel L a

a MERCK RESEARCH LABORATORIES (United States)

Author keywords

[No Author keywords available]

Indexed keywords

IMIDAZOLEMETHYL ETHER DERIVATIVE; PHENOL; PROTEIN FARNESYLTRANSFERASE; PROTEIN FARNESYLTRANSFERASE INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL MODEL; ARTICLE; CELL; CHEMICAL REACTION; CONTROLLED STUDY; DRUG ACTIVITY; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION;

ALKYL AND ARYL TRANSFERASES; ANIMALS; BINDING, COMPETITIVE; CELL LINE; ENZYME INHIBITORS; IMIDAZOLES; INHIBITORY CONCENTRATION 50; PEPTIDE LIBRARY; PHENYL ETHERS; RATS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0035927232 PISSN: 0960894X EISSN: None Source Type: Journal
DOI: 10.1016/S0960-894X(01)00162-7 Document Type: Article

Times cited : (19)

References (10)

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7
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- Distance restraints from trNOE data for 1b were used to generate conformations using JG. Kearsley, S. K., Merck & Co., Inc., unpublished.

8
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- These conformations were minimized within Macromodel using the MMFF force field with a 4r distance-dependent dielectric, and with trNOE distance constraints applied.
- These conformations were minimized within Macromodel using the MMFF force field with a 4r distance-dependent dielectric, and with trNOE distance constraints applied. Mohamadi F., Richards N.F.J., Guida W.C., Liskamp R., Caufield C., Chang G., Hendrickson T., Still W.C. J. Comput. Chem. 11:1990;440.
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9
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- One hundred conformations of 2 were generated using JG. The subsequent conformations were energy minimized with Macromodel using the procedure outlined above. The resulting energy minimized conformations were superimposed using SQ.
- One hundred conformations of 2 were generated using JG. The subsequent conformations were energy minimized with Macromodel using the procedure outlined above. The resulting energy minimized conformations were superimposed using SQ. Miller M.D., Sheridan R.P., Kearsley S.K. J. Med. Chem. 42:1999;1505.
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10
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- d of ~1 nM) in the Rat1 cell line. The nonspecific binding signal, determined by the addition of 1000-fold excess unlabeled competitor FTI, is typically 5-fold lower than the specific binding signal. The assay provides comparable results using a variety of cell lines, and is performed as follows. Cells are seeded at 200,000 cells per well in 24-well tissue culture plates and cultured for 16 h. The radiotracer (~300-1000 Ci/mmol) is diluted into culture media to a concentration of 1 nM, along with the desired
- 50 values are derived from a four-parameter curve-fitting equation using SigmaPlot® Software.
- Lobell, R.B.¹ Gibson, R.²

* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.