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. 2023 Jan 5;28(2):555. doi: 10.3390/molecules28020555

Table 2.

Antiproliferative activities of 4-PQ derivatives.

graphic file with name molecules-28-00555-i002.jpg
Compound Ring A Ring C IC50 (μM) a Against Cell Lines b
R5 R6 R7 R2’ R3’ R4’ R5’ COLO205 A498 H460 Hep3B Detroit-551
19 H H H H H H H 32.88 >50 36.49 >50 >50
20 H H H H H OCH3 H 23.33 >50 47.1 >50 >50
21 H OCH3 H H H H H >50 >50 45.7 >50 >50
22 H OCH3 H H OCH3 H H 0.32 >50 0.89 >50 >50
23 H OCH3 H H H OCH3 H >50 >50 >50 >50 >50
24 OCH3 H OCH3 H H H H >50 >50 >50 >50 >50
25 OCH3 H OCH3 H OCH3 H H 37.6 >50 46.25 >50 >50
26 OCH3 H OCH3 H H OCH3 H >50 >50 >50 >50 >50
27 OCH3 H OCH3 OCH3 H OCH3 H 7.85 >50 >50 >50 >50
28 OCH3 H OCH3 OCH3 H H OCH3 38.55 >50 32.27 ND c ND c
29 OCH3 OCH3 OCH3 H H H H >50 >50 >50 >50 >50
30 OCH3 OCH3 OCH3 H H OCH3 H >50 >50 >50 >50 >50
31 OCH3 OCH3 OCH3 OCH3 H OCH3 H >50 >50 >50 >50 >50
32 OCH3 OCH3 OCH3 OCH3 H H OCH3 >50 >50 >50 >50 >50
HPK d H -O-CH2-O- OCH3 H OCH3 H 7.4 d 48 d 0.9 d 1.0 d >25 d
PPT e 0.01 e 0.01 e 0.01 e ND c ND c
Colchicine e 0.025 e 0.03 e 0.02 e ND c ND c

a Human tumor cells were treated with different concentrations of samples for 48 h. Data are presented as the half-maximal inhibitory concentration (IC50; μM). b Cell lines included colon carcinoma (COLO205), renal cell carcinoma (A498), lung carcinoma (H460), liver carcinoma (Hep3B) and normal skin fibroblast (Detroit 551). c The data were not determined. d These data were according to a previous study [4]. e The data were downloaded from the National Cancer Institute (NCI) via the Developmental Therapeutics Program (DTP) of NCI 60 cell lines screen 5 dose–response data (https://dtp.cancer.gov/; accessed on 21 December 2022), and the data were listed in the Supplementary Materials.