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1168 Prockop, DJ. 1964. Isotopic studies on collagen degradation and the urinary excretion of hydroxyproline. Journal of Clinical Investigation. 43(3):453-460. Ranjan, R., Swarup, D. and Patra, RC. 2009. Oxidative stress indices in the erythrocytes, liver and kidneys of fluoride exposed rats. Fluoride. 42 (2):88-93. Reddy, G.K. and Enwemeka, CS. 1996. A simplified method for the analysis of hydroxyproline in biological tissues. Clinical Biochemistry. 29(3):225- 229. Saris, NL., Mervaala, E., Karppanen, H., Khawaja, JA. and Lewenstam, A. 2000. Magnesium An update on physiological, clinical and analytical aspects. Clinica chimica acta. 294:1-26. Sharma, YD. 1982 a . Effect of Sodium fluoride on collagen cross-link precursors. Toxicology Letters. 10: 97 -100. Sharma, YD. 1982 b . Variations in the metabolism and maturation of collagen after fluoride ingestion. Biochimica et Biophysica Acta. 715 (1): 137-141. Shivarajashankara, YM., Shivashankara, AR., Gopalakrishna Bhat, P. and Hanumanth Rao, S. 2002. Brain lipid peroxidation and antioxidant systems of young rats in chronic fluoride intoxication. Fluoride. 35:197- 203. Canadian Journal of Pure and Applied Sciences Siddiqi, N.J, Al-Jafari, AA. and Alhomida, AS. 2000. Investigation of total, free, peptide-bound, protein-bound, soluble- and insoluble-collagen hydroxyproline content in tissues from the Arabian camel (Camelus dromadarius). Cell Biochemistry and Function. 18:243-248. Stannard, JG., Skim, YS., Kirtsineli, M., Labropoulou, P. and Tsamtsouris, A. 1991. Fluoride Levels and Fluoride Contamination of Fruit Juices. The Journal of clinical pediatric dentistry. 16:38-40. Varghese, Z., Moorhead, JF. and Wills, MR. 1981. Plasma hydroxyproline fractions in patients with dialysis osteodystrophy. Clinica Chimica Acta. 110:105-111. Weiss, JB. and Jayson, MIV. 1982. in Collagen in Health and Disease, Churchill Livingstone, New York, USA. pp 404-405. Zabulyte, D., Uleckiene, S., Kalibatas, J., Viciene, AP., Jascaniniene, N. and Stosik M, 2007. Experimental studies on effect of sodium fluoride and nitrate on biochemical parameters in rats. Bull. Vet. Inst. Pulawy. 51:79-82. Zhao, LB., Liang, D. and Liang, WWL. 1996. Effects of a high fluoride water supply on children’s intelligence. Fluoride. 29:190-192. Received: Jan 26, 2010: Revised: April 21, 2010; Accepted: April 29, 2010
SENRA Academic Publishers, Burnaby, British Columbia Vol. 4, No. 2, pp. 1169-1178, June 2010 ISSN: 1715-9997 SYNTHESIS, CHARACTERISATION AND IN-VITRO BIOLOGICAL ACTIVITIES OF SOME METAL(II) COMPLEXES OF 3-(-1-(4-METHYL-6-CHLORO)-2-PYRIMIDINYLIMINO)METHYL-2-NAPTHOL *A A Osowole 1 , R Kempe 2 , R Schobert 3 and S A Balogun 4 1 Department of Chemistry, <strong>University</strong> of Ibadan, Ibadan, Nigeria 2 Anorganische Chemie II, Universität Bayreuth, D-95440 Bayreuth, Germany 3 Organische Chemie I, Universität Bayreuth, D-95440 Bayreuth, Germany 4 Department of Microbiology, Adekunle Ajasin <strong>University</strong> Akungba–Akoko, PMB 001 Akungba–Akoko, Ondo state, Nigeria ABSTRACT Synthesis, spectroscopic characterisation and in-vitro antibacterial and anticancer studies were done on the neutral bidentate (NO) Schiff base, 3-(-1-(4-methyl-6-chloro)-2-pyrimidinyl imino)methyl-2-napthol and its Mn(II), Co(II), Ni(II), Pd(II), Cu(II) and Zn(II) complexes. These complexes assumed a 4-coordinate tetrahedral /square-planar geometry as corroborated by room temperature magnetic data, IR and electronic spectral measurements. The conductance data confirmed their covalent nature while mass spectra and TGA data affirmed the proposed structure. The ligand was not sensitive to HL 60 (leukaemia) but resistant to 518A2 (melanoma) carcinomas. The Pd(II) complex had the best cytotoxic activities against HL 60 (Leukemia) and Melanoma (518A2) carcinomas with IC50 of 11.89 and 9.11 µm at 48 and 72 h respectively, which was a third as, and four times more sensitive than CDDP (Cis-platin). The complexes generally exhibited good antibacterial activities against five Gram negative (E. cloacae, S. arizona, Serratia sp, E. Coli) and three Gram positive (C. violaceum, S. aureus, Bacillus sp) bacteria with inhibitory zones range of 7-19 mm. Similar to gentamycin, the Cu(II) and Zn(II) complexes had broad-spectrum activity against the bacteria used, although much lower. Keywords: Antibacterial and anticancer activities, cis-platin –sensitive and –resistant cell lines, Schiff base. INTRODUCTION The interest in metal complexes as drugs has increased in the last decade due to the search for drugs with an enhanced therapeutic effect in combination with decreased toxicity (Zhaohua et al., 2001; Zhong et. al., 2006). It has been documented that drugs containing pyrimidine moiety are more prominent in treating solid tumours and cancers due to their good anti-proliferation activity and low toxicity e.g. bevacizumab in combination with 5-fluoro uracil is used in treatment of metastatic colorectal cancer (Ramaling and Belani, 2007) while sorafenib and sunitinib, which are small-molecule multikinase inhibitors are used for the treatment of advanced renal-cell carcinoma (Atkins et al., 2006; Wilhelm et al; 2006). Currently, the drug pazopanib (5- (4-[(2,3-dimethyl-2H-indazoyl-6-yl)methylamino]-2pyrimidinyl]amino-2-methyl benzene sulfonamide) is undergoing clinical development for use in treating renalcell cancer and other solid tumours (Harries et al., 2008). In addition, pyrimidinyl Schiff bases are widely studied due to their ease of preparation, coordination to many metal ions, and the stability of such oxidation states. Furthermore, their good solubility in DMSO and DMF *Corresponding author email: aderoju30@yahoo.com makes them suitable for cell lines studies (Gorneva and Golovinsky, 2003; Shreelekha et al., 2006). In continuation of our studies on synthesis, characterisation and anticancer /antimicrobial properties of some metal(II) complexes of various pyrimidinyl Schiff bases (Osowole et al., 2009), we report our findings on anticancer and antibacterial properties of Mn(II), Ni(II), Co(II), Cu(II), Zn(II) and Pd(II) complexes of 3-(-1-(4methyl-6-chloro-2-pyrimidinyl imino)methyl-2-napthol (derived from condensation of 2-amino-4-methyl-6chloropyrimidine and 2-hydroxy-1-napthaldehyde) against cis-platin–sensitive (Leukemia) and –resistant (Melanoma) cell lines and, E. cloacae, S. arizona, Serratia sp, E. Coli) and three Gram positive (C. violaceum, S. aureus, Bacillus sp). Their spectroscopic, magnetic and thermal properties are also discussed. This ligand and its metal complexes are new, being reported here by our group for the first time. MATERIALS AND METHODS Chemicals and Instrumentation All the chemicals used were of reagent grade. 2-amino-4methyl-6-chloropyrimidine and 2-hydroxy-1napthaldehyde (Across), palladium(II) chloride, hydrated manganese(II) nitrate, cobalt(II) nitrate, nickel(II) nitrate,
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