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. Author manuscript; available in PMC: 2013 Jul 15.
Published in final edited form as: Bioorg Med Chem Lett. 2012 Jun 7;22(14):4532–4535. doi: 10.1016/j.bmcl.2012.05.126

Table 1.

Structures and activities of analogs 11.

graphic file with name nihms383474t1.jpg
Cmpd R R1 % Inhib.
@ 2 µM		 IC50
(nM)
   2 H Me 82 537
11a (±)-Me Me 46 ND
11b (±)-Et Me 27 ND
11c (±)-Et Et 45 ND
11d (±)-Me Et 57 ND
11e (±)-Me graphic file with name nihms383474t2.jpg 87 570
11f a(±)-Me graphic file with name nihms383474t3.jpg ND 152
11g a(−)-Me graphic file with name nihms383474t4.jpg ND 1,900
11h (±)-Et graphic file with name nihms383474t5.jpg 84 756
11i a(+)-Et graphic file with name nihms383474t6.jpg ND 385
11j a(−)-Et graphic file with name nihms383474t7.jpg 40 ND
11k H graphic file with name nihms383474t8.jpg ND 61
11m H graphic file with name nihms383474t9.jpg ND 177
11n H graphic file with name nihms383474t10.jpg ND 1057

ND: not determined.

a

enantiomers separated by chiral SFC and (+) or (−) rotation noted,19 absolute stereochemistry is unknown.