Review Article

Copper and Its Complexes in Medicine: A Biochemical Approach

Table 3

Inhibitory effects of selected copper complexes.

ComplexBiological in vitro activityIC50  a,b (μΜ)Reference

Bis(4-nitroacetophenone thiosemicarbazonat) copper(II)Anti-trypanosomalTrypanosoma cruzi0.056 c (0.28)c[63]
Bis(5-nitrofuran-2-carboxaldehyde-N4-ethylpiperidine thiosemicarbazone) copper(II) chlorideAntiamoebicHK-9 strain of Entamoeba histolytica 0.34(2.68)[62]
Bis(thiophene-2-carboxaldehyde-N4-methyl benzyl thiosemicarbazone) copper(II) chlorideAntiamoebicHK-9 strain of Entamoeba histolytica 0.21(1.21)[62]
(2-acetylpyridine)pyridine-2-carboxamidrazone copper(II) chlorideAntiproliferativeMouse melanoma cell line B16F10.  d6.8[60]
Cu2(μ-L)2(μ-Cl)2L2Cl2L= 6-(2-chlorobenzylamino) purineAntitumorMouse melanoma B16FO8.2(85)[61]
Human malignant melanoma G36120.0[61]
(95)
Human osteogenic sarcoma HOS23 (>100)[61]
Human breast adenocarcinoma MCF724(>100)[61]
Tetra(N-methyl-1,3,5-triaza-7-phosphaadamantane copper(I) tetrafluoro borateAntitumorCervix tumor (HeLa)7.6[69]
Colon tumor (HCT-15)19.2[69]
Lung tumor (A549)8.5[69]
Melanoma (A375)16.4[69]
Bis(triphenylphosphine), dihydridobis(3-nitro-1,2,4-triazolyl)borate copper(I)AntitumorPromyelocytic leukemia (HL60)4.8[79]
Cervix carcinoma (A431)6.7[69]
Lung tumor (A549)1.5[69]
Melanoma (A375)16.4[69]

aValues refer to the most active copper (II) complex tested. Half- maximal inhibitory concentration (IC50) is a quantitative measure of the effectiveness of a compound in inhibiting a biological function as it indicates how much of a particular substance is needed to inhibit a given biological process.
bValues in parenthesis refer to the free ligand.
cThese values refer to inhibitory dose (ID50): dose that inhibits 50% of Trypanosoma cruzi growth.
dThe exponentially growing cells were counted by haemocytometer using the Trypan blue exclusion method to quantify cell viability.