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. Author manuscript; available in PMC: 2012 May 15.
Published in final edited form as: Bioorg Med Chem Lett. 2011 Mar 21;21(10):2986–2990. doi: 10.1016/j.bmcl.2011.03.047

Table 2.

Effects of N-arylmethyl substituents on integrase inhibitory potencies of hydroxy-pyrrolopyridine triones (4c) as compared with 4,5-dihydroxy-1H-isoindole-1,3(2H)-diones (3).a

graphic file with name nihms283661u2.jpg
No. R IC50 (μM)
No. IC50 (μM)
3′-Processing Strand Transfer 3′-Processing Strand Transfer
4c-1 graphic file with name nihms283661t1.jpg > 111 6.0 ± 0.7 3-1 14 ± 3 0.17 ± 0.06
4c-2 graphic file with name nihms283661t2.jpg > 111 10.4 ± 1.0 3-2 8 ± 3 5.3 ± 1.5
4c-3 graphic file with name nihms283661t3.jpg > 111 6.01 3-3 27 ± 1 0.14 ± 0.03
4c-4 graphic file with name nihms283661t4.jpg > 111 9.2 ± 1.4 3-4 25 ± 16 1.7 ± 0.8
4c-5 graphic file with name nihms283661t5.jpg > 111 > 111 3-5 72 ± 23 0.39 ± 0.21
4c-6 graphic file with name nihms283661t6.jpg > 111 90.5 ± 4.7 3-6 150 ± 36 0.72 ± 0.25
a

Data was obtained from in vitro IN assays as described in reference 4.

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