Table 3.

SAR around hit series 1 b.

Compd	R	R1	TbTryS IC50 [μm]
14	H	tBu	8.8
15	4-CF3	tBu	>100
16	3-Cl, 4-CH3	tBu	7.2
17	3-F	tBu	1.5
18	3-CF3	tBu	3.5
19	3,5-di-F	tBu	1.9
20	3,5-di-Cl	tBu	0.3
21	3,5-di-Cl	CH3	6.5
22	3,5-di-Cl	CH2CH3	2.7
23	3,5-di-Cl	N(CH3)2	0.6
24	3,5-di-F	Ph	45

[a] Conditions: NaI, K₂CO₃, DMF, 90 °C; yields: 44–86 %; the synthesis of compound 20 was previously described by Torrie et al.²⁰