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. Author manuscript; available in PMC: 2021 Nov 15.
Published in final edited form as: Bioorg Med Chem Lett. 2020 Sep 6;30(22):127520. doi: 10.1016/j.bmcl.2020.127520

Table 1.

P. falciparum growth inhibition by 1a-d, f, and indicated B- and C-ring analogs.

Entry Compound Dd2 strain P. falciparum Growth EC50 (nM)
1 1a 250 ± 70a, c
2 1b >10,000a
3 1c 3,280 ± 990a, d
4 1d 1,170 ± 60a, e
5 1f 700 ± 90a, c
6 6a >10,000
7 6b >10,000b
8 6c >10,000
9 6d >10,000b
10 8a 190 ± 30a
11 12f >10,000
12 12i >10,000
13 16a 65% inhibition at 10 μM
14 (±)-20a >10,000
15 24a ~8,000
16 25a >10,000
17 26a >10,000
a

Reported previously.10a

b

Reported previously.10b

c

100% rescued by 200 μM IPP @ 10 μM.

d

60% rescued by 200 μM IPP @ 10 μM.

e

50% rescued by 200 μM IPP @ 10 μM.

f

100% rescued by 200 μM IPP @ 2.5 μM.