1ni1 | pdb_00001ni1

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Imidazole and cyanophenyl farnesyl transferase inhibitors

File:1ni1.gif


1ni1, resolution 2.30Å

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Overview

A pyridyl moiety was introduced into a previously developed series of, farnesyltransferase inhibitors containing imidazole and cyanophenyl (such, as 4), resulting in potent inhibitors with improved pharmacokinetics.

About this Structure

1NI1 is a Protein complex structure of sequences from Rattus norvegicus with ZN, HFP and 2C5 as ligands. Full crystallographic information is available from OCA.

Reference

Discovery of potent imidazole and cyanophenyl containing farnesyltransferase inhibitors with improved oral bioavailability., Tong Y, Lin NH, Wang L, Hasvold L, Wang W, Leonard N, Li T, Li Q, Cohen J, Gu WZ, Zhang H, Stoll V, Bauch J, Marsh K, Rosenberg SH, Sham HL, Bioorg Med Chem Lett. 2003 May 5;13(9):1571-4. PMID:12699757

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