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. Author manuscript; available in PMC: 2011 May 13.
Published in final edited form as: J Med Chem. 2010 May 13;53(9):3594–3601. doi: 10.1021/jm901857d

Table 2. DART-1,3-thiazoles.

graphic file with name nihms194521u2.jpg
Compound R1 R2 IC50 (μM) TD50 (μM) TI Log TI
124 H H 1.1 ≥320 511 2.7
2 Me H 0.40 ≥320 1406 3.1
3 Me Me 0.16 38 240 2.4
4 H Me 0.37 ≥320 1520 3.2
5 Ph H 0.34 ≥320 1654 3.2
6 t-Bu H 0.25 ≥320 2249 3.4
7 Et H 0.40 ≥320 1406 3.1
8 C6H11 H 0.59 1.8 3.0 0.5
9 p- CH3Ph H 0.35 ≥320 1607 3.2
10 p-MeOPh H 0.75 19 25 1.4
11 p-MeSPh H 0.40 ≥320 1406 3.1
12 p-MeS(O2)Ph H 0.42 ≥320 1339 3.1
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