Synthesis and Preliminary Bio-evaluation of Polyaspartamide Co-conjugates of p-Amino-salicylic Acid Chelated Platinum(II) and Ferrocene Complexes
Journal of Inorganic and Organometallic Polymers and Materials
Pharmacology Division, Department of Pharmacy and Pharmacology, School of Therapeutic Sciences, University of the Witwatersrand, Johannesburg, South Africa; School of Chemistry, University of the Witwatersrand, Johannesburg, South Africa
The present study reports the preparation and preliminary biological activity results of co-conjugates of platinum ferrocene based drugs by using a novel synthetic route for the incorporation of ferrocene into the carrier. The Fe content obtained by ICP-AES was found in the range of 1.8–2.3 % by mass for the conjugates and 1.4–2.0 % by mass for the co-conjugates. The Pt content obtained by ICP-OES was in the range of 5.6–7.2 % by mass for the co-conjugates. The preliminary pharmacological evaluation performed on the MCF-7 human breast cancer cell line for conjugate 1 and 4, and corresponding co-conjugate 6 and 9 revealed that the conjugates were 5 and 2 times more active than the free drug, while the corresponding co-conjugates were 16 and 6 times more active than the free drug. © 2015, Springer Science+Business Media New York.
Atomic emission spectroscopy; Bioactivity; Cell culture; Cobalt compounds; Diseases; Organometallics; Platinum; Synthesis (chemical); Bio-evaluation; Cancer; Conjugate; Ferrocenes; Mcf-7 human breast cancer cells; Platinum drugs; Polyaspartamides; Synthetic routes; Salicylic acid