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. 2018 Feb 13;9(4):354–358. doi: 10.1021/acsmedchemlett.7b00546

Table 4. Assessment of R2, N-1 Methylbenzyl Analogues.

graphic file with name ml-2017-00546m_0008.jpg

# R2 AC40 (μM) DF30 (μM) Re (r) Re (h)
19 H 14.0 NT NT NT
20 Me 2.0 4.4 0.7 <0.2
21 Cl 0.5 0.6 0.4 <0.2
14 Br 0.3 0.4 0.4 <0.2
22 CF3 11.3 NT 0.2 <0.2
23 OMe 2.2 NT >0.7 <0.2
24 CH=CH2 1.1 1.1 >0.7 0.5
25 C≡CH 0.1 0.3 0.3 <0.2
26 C≡CCH3 >49 NT NT NT
27 CN 36.3 NT <0.2 <0.2