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. 2024 Feb 8;67(4):2849–2863. doi: 10.1021/acs.jmedchem.3c01976

Table 1. In Vitro Antitrypanosomal Potency and Cytotoxicity of Analogues 7, 11, 15, and 17.

graphic file with name jm3c01976_0011.jpg

compound R1 R2 R3 X MW cLogPa tPSAa pIC50b
                T. brucei MRC-5
2 H H O 272.3 3.1 70.1 7.2 ± 0.2 <4.2
7 Me H O 286.3 2.6 61.4 <5.0 <4.2
11 H Me   O 286.3 3.0 59.3 7.1 ± 0.1 <4.2
15 H   Me O 286.3 3.2 59.3 5.8 ± 0.1 <4.2
17 H H NH 271.3 3.5 80.5 <5.0 4.6 ± 0.0
a

cLogP and tPSA are adopted from the Collaborative Drug Discovery (CDD) Vault.

b

Mean values ± standard deviations, n ≥ 2.