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. 2023 Sep 8;28(18):6528. doi: 10.3390/molecules28186528

Table 1.

Synthetic analogs of flavones and aurones with antitumor properties.

Entry Chemical Structure Cancer Cell Lines against the Tested Compounds Present Cytotoxic Activity Ref.
1 Inline graphicFlavopiridol
  • -

    Acute myeloid leukemia cells U266 (69% growth inhibition in G0/G1 cell cycle, dosage: 100 nM).

 [44]
2 graphic file with name molecules-28-06528-i002.jpg R = OCH3
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    Cell lines of hematologic cancers RPMI8226 (99.70%), CCRFCEM (68.74%), HL60(TB) (64.01%), K562 (72.38%), MOLT4 (89.58%), SR (70.19%), growth inhibition determined at 10 µM dosage.

  • -

    Non-small-cell lung cancer (NSCLC) A549 (56.48%), HOP62 (62.50%), HOP92 (75.26%), H226 (41.45%), H23 (51.21%), H460 (69.96%), H522 (65.28%), growth inhibition determined at 10 µM dosage.

  • -

    Breast cancer cells MCF7 (65.73%), HS578T (90.80%), BT549 (73.02%), MDAMB468 (52.58%), growth inhibition determined at 10 µM dosage.

 [30]
R = OH
  • -

    Ovarian cancer cell lines OVCAR3 (76.24%), OVCAR8 (76.91%), ADRRES (50.62%) at 10 µM dosage.

  • -

    Breast cancer cells MCF7 (50.65%), HS578T (103.91%), BT549 (93.00%), MDAMB468 (40.13%), growth inhibition determined at 10 µM dosage.

3 graphic file with name molecules-28-06528-i003.jpg
  • -

    Cell lines of hematologic cancers RPMI8226 (153.74%), CCRFCEM (111.94%), HL60(TB) (65.43%), K562 (82.60%), MOLT4 (97.10%), SR (88.49%), growth inhibition determined at 10 µM dosage.

  • -

    Non-small-cell lung cancer cell lines (NSCLC) HOP92 (106.11%), H322M (56.46%), H460 (72.81%), H522 (63.27%), growth inhibition determined at 10 µM dosage.

 [30]
4 graphic file with name molecules-28-06528-i004.jpg
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    Cell lines of hematologic cancers RPMI8226 (93.25%), CCRFCEM (83.98%), HL60(TB) (42.34%), K562 (63.61%), MOLT4 (71.17%), growth inhibition determined at 10 µM dosage.

  • -

    Non-small-cell lung cancer cell lines (NSCLC) A549 (51.79%), HOP92 (100.39%), H322M (56.40%), H522 (55.74%), growth inhibition determined at 10 µM dosage.

 [30]
5 graphic file with name molecules-28-06528-i005.jpg
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    Large spectra antitumor activity:

melanoma (160.26–107.81% SKMEL5), hematologic (111.12–92.74% leukemia HL60), renal (129.05% RXF393), colon (98.27–82.03% COLO205), lung (93.28% H522), brain (147.04–141.63% SF295 glioma), ovarian (76.54–51.79% IGROV1, OVCAR3, OVCAR8, ADREES, SKOV3), growth inhibition determined at 10 µM dosage. 		[31]
6 graphic file with name molecules-28-06528-i006.jpg
  • -

    Androgen-sensitive prostate cancer cell line LNCaP (IC50 = 2.4 ± 1.5 µM).

  • -

    Androgen-insensitive prostate cancer cell lines PC-3 (IC50 = 1.4 ± 0.2 µM) and DU145 (IC50 = 7.6 ± 2.4 µM).

 [32]
7 graphic file with name molecules-28-06528-i007.jpg
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    Breast cancer cell lines MCF-7 (IC50 = 3.65 ± 0.021 µM), Hs578T (IC50 = 4.52 ± 0.019 µM), with tumor selectivity compared to non-cancer cell lines MCF-10A (4.17 and 3.08).

 [10]
8 graphic file with name molecules-28-06528-i008.jpg
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    Non-small cell lung cancer cell lines: HOP-62 (GI50 = 3.76 µM), HOP-92 (GI50 = 4.43 µM), NCI-H226 (GI50 = 3.51 µM), NCI-H23 (GI50 = 7.70 µM), NCI-H522 (GI50 = 6.60 µM).

  • -

    Colon cancer cell line: HCT-116 (GI50 = 5.91 µM).

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    Central nervous system cancer cell lines: SF-268 (GI50 = 4.32 µM), SF-539 (GI50 = 5.17 µM), SNB-19 (GI50 = 4.51 µM), SNB-75 (GI50 = 3.74 µM).

  • -

    Melanoma: MALME-3M (GI50 = 5.06 µM), SK-MEL-2 (GI50 = 6.80 µM).

  • -

    Ovarian cancer cell lines: OVCAR-8 (GI50 = 3.76 µM), NCI/ADR-RES (GI50 = 5.57 µM), SK-OV-3 (GI50 = 6.57 µM).

  • -

    Renal cancer cell lines: 786-0 (GI50 = 9.26 µM), ACHN (GI50 = 6.23 µM), CAKI-1 (GI50 = 5.76 µM), RXF 393 (GI50 = 3.58 µM).

  • -

    Breast cancer cell lines: HS 578T (GI50 = 6.26 µM), BT-549 (GI50 = 7.98 µM).

 [33]
9 graphic file with name molecules-28-06528-i009.jpg
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    Non-small cell lung cancer cell lines: HOP-62 (GI50 = 2.33 µM), HOP-92 (GI50 = 1.89 µM), NCI-H226 (GI50 = 2.07 µM), NCI-H23 (GI50 = 3.70 µM), NCI-H522 (GI50 = 3.66 µM).

  • -

    Colon cancer cell line: HCT-116 (GI50 = 3.52 µM).

CNS cancer: SF-268 (GI50 = 3.52 µM), SF-295 (GI50 = 2.32 µM), SF-539 (GI50 = 2.21 µM), SNB-19 (GI50 = 4.55 µM), SNB-75 (GI50 = 1.69 µM), U251 (GI50 = 2.80 µM).
  • -

    Melanoma: MALME-3M (GI50 = 2.03 µM), SK-MEL-2 (GI50 = 4.49 µM).

  • -

    Ovarian cancer cell line: IGROV1 (GI50 = 4.45 µM).

  • -

    Renal cancer cell lines: 786-0 (GI50 = 1.96 µM), RXF 393 (GI50 = 1.78 µM), TK-10 (GI50 = 3.01 µM).

  • -

    Breast cancer cell lines: MDA-MB-231/ATCC (GI50 = 2.34 µM), HS 578T (GI50 = 3.28 µM), MDA-MB-468 (GI50 = 1.97 µM).

 [33]
10 graphic file with name molecules-28-06528-i010.jpg
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    Non-small cell lung cancer cell lines: A549 (IC50 = 4.2 ± 0.4 µM), NCI-H1975 (IC50 = 2.3 ± 0.2 µM).

 [34]
11 graphic file with name molecules-28-06528-i011.jpg
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    Human adenocarcinoma cell line A549 (IC50 = 39.17 µM).

 [35]
12 graphic file with name molecules-28-06528-i012.jpg
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    Human adenocarcinoma cell line A549 (IC50 = 39.21 µM).

 [35]
13 graphic file with name molecules-28-06528-i013.jpg
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    Human adenocarcinoma cell line A549 (IC50 = 48.43 µM).

 [35]
14 graphic file with name molecules-28-06528-i014.jpg
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    Human adenocarcinoma cell line A549 (IC50 = 43.48 µM).

 [35]
15 graphic file with name molecules-28-06528-i015.jpg
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    AR-negative castration-resistant prostate cancer cell line (CRPC) as topoisomerase II catalytic inhibitor (88.9% growth inhibition at 20 µM) and by intercalating and binding to the DNA minor groove (IC50 = 0.13 ± 0.007 µM).

  • -

    Sensitizes AR-positive CRPC cells to enzalutamide and taxanes.

 [45]
16 graphic file with name molecules-28-06528-i016.jpg
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    Human pancreas adenocarcinoma ascites metastasis Aspc-1 cancer cell lines (IC50 = 5.30 µM).

 [46]
17 graphic file with name molecules-28-06528-i017.jpg
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    MCF-7 breast cancer cells (IC50 = 5.6 ± 1.94 µM) and yeasts expressing human caspase-7.

 [11]
18 graphic file with name molecules-28-06528-i018.jpg
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    Human erythroleukemia cell line HEL (IC50 = 9.945 ± 0.930 µM).

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    Prostate cancer cell line PC3 (IC50 = 6.473 ± 0.811 µM).

 [47]
19 graphic file with name molecules-28-06528-i019.jpg
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    Human erythroleukemia cell line HEL (IC50 = 7.563–8.886 µM).

  • -

    Prostate cancer cell line PC3 (IC50 = 9.140–10.242 µM).

 [47]
20 graphic file with name molecules-28-06528-i020.jpg
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    Human erythroleukemia cell line HEL (IC50 = 10.526 ± 0.992 µM).

  • -

    Prostate cancer cell line PC3 (IC50 = 11.266 ± 0.971 µM).

 [47]
21 graphic file with name molecules-28-06528-i021.jpg
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    Leukemia cell line, doxorubicin-resistant phenotype CEM/ADR5000 (IC50 = 5.85 ± 0.46 µM).

 [43]
22 graphic file with name molecules-28-06528-i022.jpg
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    Breast adenocarcinoma cell line, resistant phenotype MDA-MB231/BCRP (IC50 = 5.43 ± 3.17 µM).

 [43]
23 graphic file with name molecules-28-06528-i023.jpg
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    Human colorectal cancer cell line HCT 116 (IC50 = 36 µM).

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    Human chronic myelogenous leukemia cell line K562 (IC50 = 23 µM).

  • -

    Hormone-dependent breast cancer cell line MCF-7 (IC50 = 23 µM).

 [48]
24 graphic file with name molecules-28-06528-i024.jpg
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    Human chronic

    myelogenous leukemia cell line K562 (IC50 = 20 µM).

 [48]
25 graphic file with name molecules-28-06528-i025.jpg
  • -

    Inhibition of in vitro angiogenesis of HUVEC (human umbilical vein endothelial cells) proliferation, motility, and tube

    formation (IC50 = 0.25 µM).

  • -

    Anti-proliferative and anti-invasive

    activities against A549 (non-small cell lung cancer cell line, IC50 = 1.25 µM), and MCF-7 (breast cancer cell line, IC50 = 1.81 µM).

 [49]
26 graphic file with name molecules-28-06528-i026.jpg
  • -

    Inhibition of in vitro angiogenesis of HUVEC (human umbilical vein endothelial cells) proliferation, motility, and tube formation (IC50 = 0.23 µM).

  • -

    Anti-proliferative and anti-invasive

    activities against A549 (non-small cell lung cancer cell line, IC50 = 1.29 µM), and MCF-7 (breast cancer cell line, IC50 = 2.95 µM).

 [49]
27 graphic file with name molecules-28-06528-i027.jpg
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    Leucocythemia cell line HL-60 (IC50 = 1.54–3.53 µM).

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    Colorectal adenocarcinoma cell line HT-29 (IC50 = 4.12–8.90 µM).

 [50]
28 graphic file with name molecules-28-06528-i028.jpg
  • -

    Human oral squamous carcinoma cell lines Ca9-22 (derived from gingival tissue, CC50 = 37 µM), HSC-2 (CC50 = 57 µM), and HSC-4 (derived from tongue, CC50 = 31 µM), with tumor-specificity in comparison to oral normal cells.

 [51]
29 graphic file with name molecules-28-06528-i029.jpg R = Cl: leukemia cell lines MOLT-4 (−17.79% mean growth percentage), and SR (−22.38% mean growth percentage).
R = H: renal cancer cell line UO-31 (−44.36% mean growth percentage).
The mean growth percentages were determined for five concentrations ranging from 10−4 to 10−8 M. 		[52]
30 graphic file with name molecules-28-06528-i030.jpg
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    Gastric cancer cell line CRL-1739.

R′ = CH3 and R = CH3, OCH3, NO2 (IC50 = 25–28.3 µM).
R′ = NO2 and R = NO2 (IC50 = 25.1 µM).		 [53]
31 graphic file with name molecules-28-06528-i031.jpg
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    Gastric cancer cell line CRL-1739 (IC50 = 27.0 µM).

 [53]