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. Author manuscript; available in PMC: 2013 Jan 12.
Published in final edited form as: J Med Chem. 2011 Dec 29;55(1):367–377. doi: 10.1021/jm201251c

Table 1.

QR2 Inhibitory Activities of Ammosamide B and Tricyclic Analogues 30-32

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Compd -R1 -R2 -R3 -R4 -R5 IC50 (μM) % max Inhibition
2 (Ammosamide B) -CH3 -NH2 -Cl -NH2 -C(=O)NH2 0.061 ± 0.005 90.3 ± 1.3
30 -CH3 -Cl -H -Cl -C(=O)NH2 5.8 ± 1.2 46.3 ± 2.4
31 -CH3 -Cl -H -Cl -C(=O)NH-CH2-Ph 7.8 ± 1.2 44.8 ± 2.0
32 -CH3 -Cl -H -Cl -C(=O)N(CH3)2 25.2 ± 9.4 31.5 ± 4.6
38 -CH3 -NH2 -Cl -NHCH3 -C(=O)NH2 0.0041 ± 0.0002 101.9±1.1