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. Author manuscript; available in PMC: 2022 Feb 21.
Published in final edited form as: J Med Chem. 2018 May 14;61(12):5162–5186. doi: 10.1021/acs.jmedchem.7b01862

Table 6.

Biological Activity of Naphthyridinesa

graphic file with name nihms-1775450-t0058.jpg
DHODH Assay MTT Assay
# R1 R2 IC50 (μM) cLogP LipE HCT-116 IC50 (μM) MIA PaCa-2 IC50 (μM)
32 graphic file with name nihms-1775450-t0059.jpg Me 0.0754 ± 0.017 5.66 1.46 8.51 ± 2.0 5.29 ± 1.1
45 graphic file with name nihms-1775450-t0060.jpg Me 1.22 ± 0.49 4.16 1.75 > 100 > 100
46 graphic file with name nihms-1775450-t0061.jpg Me 0.0283 ± 0.0033 4.16 3.39 6.30 ± 7.0 4.50 ± 3.2
47 graphic file with name nihms-1775450-t0062.jpg Me 2.79 ± 1.3 4.16 1.39 26.7 ± 11 28.1 ± 8.1
48 graphic file with name nihms-1775450-t0063.jpg Me 0.0212 ± 0.0039 5.04 2.63 0.880 ± 0.13 2.18 ± 1.7
a

Data for cLogP values was predicted using ChemBioDraw Professional 16. Lipophilic ligand efficiency (LipE) calculated LipE = −pIC50 (M) – cLogP.33