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. Author manuscript; available in PMC: 2012 Apr 14.
Published in final edited form as: J Med Chem. 2011 Mar 7;54(7):2282–2292. doi: 10.1021/jm1014378

Table 6.

Fold-resistance of inhibitors 4 and 13 against raltegravir-resistant HIV-1 strains

Viruses Major Mutations Fold-resistancea
4b 13c 1
8070-2 G140S/Q148H 7.3 >2.0 >855
1556-1 Y143C 5.9 >1.7 >855
4736-2 N155H 3.1 >5.1 149
a

Fold-resistance is defined by EC50(mutant)/EC50 (WT).

b

Ref 30.

c

Toxicity observed (TC50 = 2.0 μM).