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. Author manuscript; available in PMC: 2021 Apr 23.
Published in final edited form as: J Med Chem. 2020 Apr 8;63(8):4256–4292. doi: 10.1021/acs.jmedchem.0c00193

Table 5.

PI3K/HDAC Enzyme Inhibitory Activities of 5-Substituted Quinazolinones with Amino-pyrimidine Hinge Bindersa

IC50 (nM) HDAC6 isoform selectivityb
Compound L R1 R2 PI3K HDAC6
α β γ δ
46a graphic file with name nihms-1582028-t0005.jpg Et graphic file with name nihms-1582028-t0006.jpg 52 33 3 0.7 69 >13
46b graphic file with name nihms-1582028-t0007.jpg Et graphic file with name nihms-1582028-t0008.jpg 9 12 2 0.2 28 >36
46c graphic file with name nihms-1582028-t0009.jpg Et graphic file with name nihms-1582028-t0010.jpg 5210 1769 96 45 >22
46d graphic file with name nihms-1582028-t0011.jpg Et graphic file with name nihms-1582028-t0012.jpg 13 26 2 0.2 77 >7
48a graphic file with name nihms-1582028-t0013.jpg Et graphic file with name nihms-1582028-t0014.jpg 186 279 8 5 1238 >2
48b graphic file with name nihms-1582028-t0015.jpg Et graphic file with name nihms-1582028-t0016.jpg 50 842 45 32 4 >73
48c graphic file with name nihms-1582028-t0017.jpg Et graphic file with name nihms-1582028-t0018.jpg 47 9 7.0 12 >39
48d graphic file with name nihms-1582028-t0019.jpg Et graphic file with name nihms-1582028-t0020.jpg 4 >58
48e graphic file with name nihms-1582028-t0021.jpg Et graphic file with name nihms-1582028-t0022.jpg 444 752 60 4 >113
48f graphic file with name nihms-1582028-t0023.jpg Et graphic file with name nihms-1582028-t0024.jpg 133 4 >5
48g graphic file with name nihms-1582028-t0025.jpg Et graphic file with name nihms-1582028-t0026.jpg 189 3 >81
48h graphic file with name nihms-1582028-t0027.jpg Et graphic file with name nihms-1582028-t0028.jpg 663 22 >15
48i graphic file with name nihms-1582028-t0029.jpg Et graphic file with name nihms-1582028-t0030.jpg 491 14 >20
48j graphic file with name nihms-1582028-t0031.jpg Et graphic file with name nihms-1582028-t0032.jpg 269 9 >24
48k graphic file with name nihms-1582028-t0033.jpg Et graphic file with name nihms-1582028-t0034.jpg 52 >13
481 graphic file with name nihms-1582028-t0035.jpg Et graphic file with name nihms-1582028-t0036.jpg 47 >9
48m graphic file with name nihms-1582028-t0037.jpg Et graphic file with name nihms-1582028-t0038.jpg 222 390 27 >6
48n graphic file with name nihms-1582028-t0039.jpg Me graphic file with name nihms-1582028-t0040.jpg 42 159 4 4 6 >31
48o graphic file with name nihms-1582028-t0041.jpg Me graphic file with name nihms-1582028-t0042.jpg 75 188 2 4 8 >15
51 graphic file with name nihms-1582028-t0043.jpg Me graphic file with name nihms-1582028-t0044.jpg 18 379 10 0.7 16 >6
54 graphic file with name nihms-1582028-t0045.jpg Me graphic file with name nihms-1582028-t0046.jpg 42 293 15 3 3 >25
PI-103 - - - 4 7 55 5 NT -
TSA - - - NT NT NT NT 6 -
TMP269 - - - NT NT NT NT NT -