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. 2020 Apr 10;25(7):1757. doi: 10.3390/molecules25071757

Table 1.

Structures and mechanism of action DNA-binding vanadium compounds (Kb-binding constant).

Structure Activity References
graphic file with name molecules-25-01757-i001.jpg Groove binding to salmon sperm DNA accompanied with a partial insertion between the base stacks of the DNA
(Kb = 2.3 × 103 M−1)
Cytotoxicity (24 h):
breast cancer cells MCF-7 (IC50 7.8 µM)
liver cancer cells HepG2 (IC50 13.5 µM)
colon cancer cells HT-29 (IC50 16.1 µM)		 [25]
graphic file with name molecules-25-01757-i002.jpg Oxidative cleavage of DNA through the generation of a hydroxyl radical
Minor groove binding to DNA
(2: Kb = 1.95 ± 0.16 × 103 M−1
3: Kb = 1.064 ± 0.17 × 103 M−1)
Cytotoxicity (48 h):
cervical cancer cells HeLa
(2: IC50 256.9 µM 3: IC50 480.5 µM)		 [26]
graphic file with name molecules-25-01757-i003.jpg Similarities to cisplatin concerning DNA interaction
ROS generation, mitochondrial damage, G2/M cell cycle arrest
Cytotoxicity (72 h):
panel of melanoma, colon, cervical, breast and pancreatic cancer cells
IC50 < 10 µM for all cell lines 		[27]
graphic file with name molecules-25-01757-i004.jpg Intercalation as the way of DNA binding
G2/M cell cycle arrest
Cytotoxicity (48 h):
cervical cancer cells HeLa
(5: IC50 42.9 ± 1.5 µM
6: IC50 33.2 ± 0.9 µM)
breast cancer cells T-47D
(5: IC50 38.0 ± 1.6 µM
6: IC50 42.3 ± 1.8 µM)
Lung cancer cells A549
(5: IC50 87.6 ± 2.4 µM
6: IC50 > 100 µM)		 [28]
graphic file with name molecules-25-01757-i005.jpg Phen-containing VIVO compounds display stronger DNA interaction ability than the corresponding bipy analogues
Cytotoxicity (72 h):
ovarian cancer cells A2780
(7: IC50 20.8 ± 0.5 µM 8: IC50 4.9 ± 1.3 µM
9: IC50 17.1 ± 3.9 µM 10: IC50 4.7 ± 1.8 µM)
breast cancer cells MCF-7
(7: IC50 53 ± 2.0 µM 8: IC50 77 ± 1.3 µM
9: IC50 95 ± 3.7 µM 10: IC50 68 ± 1.4 µM)		 [29]
graphic file with name molecules-25-01757-i006.jpg Interaction with CT-DNA through a non-classical intercalative mode
cleavage plasmid pBR322 DNA upon exposure to ultraviolet light
Cytotoxicity (48 h):
panel of cervical, breast and esophageal cancer cells
IC50 range: 0.31–6.15 μM 		[30]
graphic file with name molecules-25-01757-i007.jpg Binding with CT-DNA by an intercalation
Kb = 14: 1.53 × 105 M−1 15: 1.41 × 105 M−1
16: 1.05 × 105 M−1 17: 0.95 × 105 M−1
cleave supercoiled plasmid DNA in the presence of H2O2
G0/G1 cell cycle arrest (14)
Induction apoptosis in Hela cells (14)
Cytotoxicity (24 h):
cervical cancer cells HeLa
(14: IC50 1.09 ± 0.16 µM
15: IC50 10.36 ± 1.23 µM)
bladder cancer cell BIU-87
(14: IC50 4.51 ± 0.68 µM
15: IC50 8.69 ± 1.05 µM)
lung cancer cells SPC-A-1
(14: IC50 7.61 ± 0.55 µM
15: IC50 21.43 ± 3.24 µM)		 [31]
graphic file with name molecules-25-01757-i008.jpg Interaction with DNA in a intercalative fashion (Kb = 2.76 × 105 M−1)
Cytotoxicity (24 h):
lung cancer cell A549
breast cancer cells MCF-7
keratinocyte cancer cell A431
IC50 for all cancer cell lines 75 μM
normal human keratinocyte cells HaCaT
IC50 150 µM 		[32]
graphic file with name molecules-25-01757-i009.jpg The intercalative mode of binding to DNA
(19: Kb = 6.13 × 105 M−1
20: Kb = 8.69 × 105 M−1)
Cytotoxicity (24 h):
cervical cancer cell SiHa
(19: IC50 33 µM 20: IC50 29 µM)		 [33]
graphic file with name molecules-25-01757-i010.jpg Binding to CT-DNA
Kb = 21: 6.10 × 104 M−1 22: 7.99 × 104 M−1
23: 6.75 × 104 M−1 24: 6.07 × 104 M−1
25: 8.80 × 104 M−1
Cytotoxicity (48 h):
breast cancer cells MCF-7
(25: IC50 11.44 µM 23: IC50 15.50 µM)
liver cancer cells HepG2
(25: IC50 9.91 µM 23: IC50 11.01 µM)
colon cancer cells HCT 116
(24: IC50 13.27 µM 23: IC50 15.53 µM)		 [34]
Inline graphic
Inline graphic 		Light-activated VO2+-DNA crosslink formation (27)
singlet oxygen (1O2) induced mitochondria-targeted PDT (27)
Cytotoxicity (24 h):
breast cancer cells MCF-7
(27: IC50 3.4±0.4 µM in visible light
IC50 > 50 µM in the dark)
cervical cancer cells HeLa
(27: IC50 1.8±0.6 µM in visible light
IC50 > 50 µM in the dark)
26: any significant cytotoxicity in light		 [36]
graphic file with name molecules-25-01757-i013.jpg Light-activated DNA crosslink formation (in the dark they are partial DNA intercalators)
ROS generation in visible light
Cytotoxicity (24 h):
breast cancer cells MCF-7
(28: IC50 10.4 ± 1.6 µM in visible light
IC50 > 50 µM in the dark)
(29: IC50 2.3 ± 0.3 µM in visible light
IC50 27.6 ± 1.4 µM in the dark)
cervical cancer cells HeLa
(28: IC50 8.2 ± 0.3 µM in visible light
IC50 > 50 µM in the dark)
(29: IC50 1.8 ± 0.5 µM in visible light
IC50 20.3 ± 1.0 µM in the dark)		 [37]
Inline graphic
Inline graphic 		Photo-induced cleavage of pUC19 supercoiled plasmid DNA
Interaction with CT-DNA through minor groove binding mode
Kb = 30: 8.56 × 104 M−1 31: 1.13 × 105 M−1
32: 4.95 × 104 M−1 33: 5.03 × 103 M−1
Cytotoxicity (72 h):
cervical cancer cells HeLa
30: IC50 20 ± 4.52 µM
31: IC50 18 ± 3.38 µM
32: IC50 19.5 ± 3.54 µM
33: IC50 9.9 ± 3.18 µM 		[38]
graphic file with name molecules-25-01757-i015.jpg The topoisomerase IB inhibition (34)
G2/M cell cycle arrest (35)
activation caspase 3 and triggering the apoptosis (34)
Cytotoxicity (24 h):
colon cancer cells HT-29
A concentration-related inhibition
from 75 to 100 µM 		[40]

Bold and Underline: makes Table more readable.