SYNTHESIS, CHARACTERISATION, CYTOTOXIC ACTIVITY EVALUATION AND STRUCTURE-ACTIVIITY RELATIONSHIP STUDY OF NEW FERROCENE-INDOLE DERIVATIVES AS POTENTIAL ANTICANCER AGENTS

Abstract

Ferrocene-indole is a series of organometallic molecules that consist of a ferrocene moiety directly or indirectly attached to an indole core at any possible position of substitution. A series of seven new ferrocene-indole molecules was synthesised, designed and their cytotoxicity were tested against cancer cell lines. The study concludes that ferrocene-indole with indole substituted at position 2 and 7 are more active in cytotoxicity compared to the others in the series. The employed synthesis method was a resemblance of Steglich Esterification, with EDC·HCl acted as coupling agent and DMAP as catalyst. A precursor molecule, ferrocenephenylenediamine was synthesised through EDC coupling. In addition, a series of ferrocenephenyldiamide-indole was synthesised using the mentioned precursor, with all six possible indoles substituted by the precursor. Characterisation of the compounds were accomplished by Nuclear Magnetic Resonance (NMR), Fourier-Transform Infrared Spectroscopy (FT-IR), CHN Elemental Analysis and Mass Spectroscopy (MS). Meanwhile, MTS Assay was chosen as a biological evaluation of the six ferrocene-indole hybrids.