. Author manuscript; available in PMC: 2014 Sep 15.

Published in final edited form as: Bioorg Med Chem Lett. 2013 Jul 8;23(18):5209–5212. doi: 10.1016/j.bmcl.2013.06.093

Table 1.

Anti-HIV-1 Activity (EC₅₀) and cytotoxicity (CC₅₀), μM^a

Compound	R	R′	EC₅₀	CC₅₀
2a^b	OCH₃	H	0.011	42
2b^b	OCH₃	OCH₃	0.022	>100
2c^c	OCH₃	OCH₂CH₂OCH₃	0.097	8.6
2d^c	CH₂CH₃	OCH₂CH₂OCH₃	0.057	2.1
2e^c	OCH₃	(OCH₂CH₂)₃OCH₃	0.380	4.2
2f	OCH₃	(OCH₂CH₂)₄NH₂	2.2	23
2g	OCH₃	(OCH₂CH₂)₆NH₂	5.0	18
2h^c	OCH₃	OCH₂CH₂-4-MePiz	0.320	7.0
2i^c	OCH₃	OCH₂CH₂-2-THP	1.2	4.2
2j	OCH₃	OCH₂CH₂-Morph	0.092	2.5
2k	OCH₃	OCH₂CH₂CH₂-Morph	0.095	3.6
2l	CH₂CH₃	OCH₂CH₂-Morph	0.150	0.8
2m	c-C₃H₅	OCH₂CH₂-Morph	0.100	0.9
2n	OCH₃	OCH₂CH₂CH₂-4-Pip	1.500	5.6
nevirapine			0.110	>100
efavirenz			0.002	15
rilpivirine			0.001	8

4-MePiz = N-methylpiperazinyl; 2-THP = 2-tetrahydropyranyl (racemic); Morph = N-morpholinyl; Pip = piperidinyl.

Ref. 10.

Ref. 16.