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. Author manuscript; available in PMC: 2014 Feb 14.
Published in final edited form as: J Med Chem. 2013 Jan 30;56(3):1007–1022. doi: 10.1021/jm301485d

TABLE 1.

In Vitro Neuroprotective Activity of 1,4-naphthoquinones substituted at the 2′ and 3′ positions.

graphic file with name nihms438563u1.jpg
Compound R1 R2 Protectiona Toxicityb Safety Index
PC50 (nM) TC50 (nM) TC50/PC50
VK2 - - 432 >100,000 231
1a -H -H 1541 19,000 12
1b -Me -H 797 19,000 24
1c -Me -Me 118 30,000 254
1d -NH2 -H 61 49,000 803
1e -NH2 -Me 1740 54,000 31
1f -COOH -H 716 >100,000 140
1g -OH -H 1005 >100,000 100
a

In vitro neuroprotective activity and

b

neurotoxicity assessed by treating HT22 cells with various concentrations of compounds with or without 10 mM glutamate for 24 hrs. Cell viability was estimated by treating cells with MTS and measuring absorbance at 490 nM. PC50, concentration producing 50% protection, values calculated using GraphPad Prism based on 12 point titrations, n ≥ 4; TC50, concentration producing 50% toxicity, values calculated using GraphPad Prism based on 7 point titrations, n ≥ 3.