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. Author manuscript; available in PMC: 2012 Dec 1.
Published in final edited form as: Bioorg Med Chem Lett. 2011 Oct 1;21(23):7170–7174. doi: 10.1016/j.bmcl.2011.09.073

Table 1.

Antiproliferative activity of non-labile novobiocin analogs.

graphic file with name nihms328781u2.jpg
Entry X R R1 R2 SkBR3 MCF7
13 O a OMe H 19.51±1.8 18.20±2.1
14 O b OMe H 42.72±2.1 6.51±0.7
15 O a H OMe 13.68±1.1 15.69±2.3
16 O b H OMe 33.14±0.9 62.8±4.4
17 O a tBu H 72.39±1.9 74.99±4.9
18 O b tBu H 68.27±3.8 20.55±0.8
19 O c OMe H >100 >100
20 O c H OMe >100 >100
21 O c tBu H >100 >100
30 NH a OMe H >100 >100
31 NH b OMe H >100 >100
32 NH c OMe H >100 >100
43 CH2 a OMe H 23.49±0.7 11.5±0.9
44 CH2 b OMe H 11.08 13.25±1.2
46 CH2 b H OMe 14.83±1.3 19.65±2.0
48 CH2 b OMe OMe >100 13.94±3.3
49 CH2 a OMOM OMe 14.24±0.4 14.88±0.9
50 CH2 b OH OMe 10.69±1.1 14.62±1.4
51 CH2 a OMOM H 13.50±0.7 22.67±1.7
52 CH2 b OH H 21.46±0.5 32.11±3.2
53 CH2 c H H 4.09±0.2 7.11±1.6
54 CH2 c OMe H >100 >100