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. 2022 Jun 8;10:888727. doi: 10.3389/fchem.2022.888727

TABLE 1.

Inhibitory activities of 2,5-substituted furan derivatives 1a–k against PRMT1.

graphic file with name fchem-10-888727-fx1.jpg
Cpd no. Cpd ID. R1 R 2 % Inhibition of PRMT1 (at 10 μM) a IC50 (μM)
SAH 0.55 ± 0.07
DB75 98.13 ± 0.27 0.31 ± 0.04
1a ZZQ-16 H -CONH2 10.61 ± 2.24
1b ZZQ-82 H -CONHNH2 48.00 ± 0.02
1c ZZQ-55 H -NH2 50.00 ± 0.18 21.42 ± 12.76
1d ZZQ-52 -NH2 H 35.99 ± 0.09
1e ZZQ-102 H graphic file with name fchem-10-888727-fx2.jpg 32.00 ± 0.00
1f ZZQ-127 F graphic file with name fchem-10-888727-fx3.jpg 35.97 ± 0.20
1g ZZQ-100 graphic file with name fchem-10-888727-fx4.jpg H 39.98 ± 0.19
1h SYT-302 H graphic file with name fchem-10-888727-fx5.jpg 74.54 ± 0.16 2.66 ± 0.01
1i SYT-298 F graphic file with name fchem-10-888727-fx6.jpg 68.00 ± 0.02 4.42 ± 0.63
1j SYT-290 graphic file with name fchem-10-888727-fx7.jpg H 76.82 ± 1.19 2.06 ± 0.60
1k SYT309 graphic file with name fchem-10-888727-fx8.jpg Cl 76.50 ± 0.01 2.50 ± 0.91
a

Initial inhibition rate was tested at 10 μM for all compounds, and only those with >50% inhibition effects were selected for IC50 measurements.