Synthesis and anticancer activity of certain mononuclear Ru (II) Complexes

Figures & data

Scheme 1 Preparation of cis-Ru(phen)₂Cl₂ and cis-Ru(bpy)₂Cl₂

Scheme 2 Preparation of tris chelates from cis-Ru(phen)₂Cl₂ and cis-Ru(bpy)₂Cl₂

Figure 1 Structures of the ruthenium(II) complexes.

Table I.  Anticancer activity of ruthenium complexes against EAC-bearing mice.

Treatment	Total body weight (g)	Mean survival time (days)	ILS (%)	Tumor volume (ml)	Viable cells in ascitic fluid (%)
Group I	21.4 ± 0.9	–	–	–	–
Group II	28.0 ± 1.5	22	–	3.4 ± 0.3	96.5 ± 1.4
Group III	18.5 ± 0.6	23	5	–	–
Group IV	23.1 ± 0.9	38	73	0.8 ± 0.2	47.0 ± 1.7
Group V	22.1 ± 1.1	35	59	0.8 ± 0.3	45.6 ± 3.0
Group VI	24.4 ± 0.7	27	23	1.8 ± 0.3	67.5 ± 1.9
Group VII	25.1 ± 0.9	30	36	1.8 ± 0.3	75.4 ± 2.6
Group VIII	24.8 ± 0.3	31	41	1.5 ± 0.2	64.6 ± 1.5
Group IX	23.6 ± 0.8	25	14	1.4 ± 0.3	64.9 ± 2.2

Values are mean ± SEM.Group I: Vehicle (5 ml/kg); Group II: EAC (2 × 10⁶ cells/mouse); Group III: Cisplatin (2 mg/kg) + EAC; Group IV-IX: Ruthenium complexes (2 mg/kg) + EAC.

Table II.  Effect of ruthenium complexes on the hematological profile of EAC-bearing mice.

Treatment	Hemoglobin (g/dl)	RBC (cell count × 10^8)	WBC (cell count × 10^6)	Lymphocyte (%)	Monocyte (%)	Granulocyte (%)
Group I	12.2 ± 0.4	12.6 ± 0.5	6.6 ± 0.3	71.8 ± 0.5	2.6 ± 0.4	26.1 ± 0.6
Group II	10.0 ± 0.6	6.6 ± 0.6	17.7 ± 0.6	62.7 ± 0.7	33.4 ± 0.4	4.6 ± 0.5
Group III	11.0 ± 0.7	4.9 ± 0.7	10.8 ± 0.3	66.0 ± 0.78	29.4 ± 0.3	5.2 ± 0.2
Group IV	11.7 ± 0.6	6.7 ± 0.4	9.2 ± 0.8	77.8 ± 0.5	5.3 ± 0.2	18.0 ± 0.7
Group V	12.2 ± 0.6	6.0 ± 0.4	9.7 ± 0.7	77.0 ± 0.7	4.7 ± 0.1	17.5 ± 0.6
Group VI	10.2 ± 0.8	5.9 ± 0.8	11.9 ± 0.4	80.2 ± 0.7	8.7 ± 0.2	11.7 ± 0.4
Group VII	9.4 ± 0.9	5.8 ± 0.8	10.8 ± 0.9	81.0 ± 0.4	8.2 ± 0.2	11.8 ± 0.4
GroupVIII	9.8 ± 0.6	6.1 ± 0.6	10.7 ± 0.6	80.2 ± 1.0	7.3 ± 0.2	13.3 ± 0.6
Group IX	8.9 ± 0.5	5.6 ± 0.5	10.9 ± 0.9	79.0 ± 0.5	7.3 ± 0.2	14.6 ± 0.8

Values are mean ± SEM.Group I: Vehicle (5 ml/kg); Group II: EAC (2 × 10⁶ cells/mouse); Group III: Cisplatin (2 mg/kg) + EAC; Group IV–IX: Ruthenium complexes (2 mg/kg) + EAC.

Table III.  IC₅₀ value of synthesized ruthenium complexes in the antihemolytic activity assay.

Synthesized complexes	IC50 Values (μg/ml)
Ru Complex – 1	76.15
Ru Complex – 2	73.28
Ru Complex – 3	89.62
Ru Complex – 4	94.37
Ru Complex – 5	85.51
Ru Complex – 6	84.24