Synthesis of a 1,4-benzodiazepine containing palladacycle with in vitro anticancer and cathepsin B activity
Spencer, John, Rathnam, Rajendra P., Montukuri, Mahesh, Kotha, Arun K., Richardson, Simon C.W., Hazrati, Ali, Hartley, John A., Male, Louise and Hursthouse, Michael B. (2009) Synthesis of a 1,4-benzodiazepine containing palladacycle with in vitro anticancer and cathepsin B activity. Dalton Transactions (22). pp. 4299-4303. ISSN 1477-9226 (Print), 1477-9234 (Electronic) (doi:10.1039/b819061e)Full text not available from this repository.
The reaction of the five-membered C,N-palladacycle [(L)PdCl](2), where LH = 1-methyl-5-phenyl-1H-1,4-benzodiazepin-2(3H)-one, with 1,2-ethanebis(diphenylphosphine), dppe, leads to the formation of the bridged palladacycle. [Pd(2)L(2)(mu-dppe)Cl(2)] 3, which was characterised in solution by (1)H and (31)P NMR spectroscopy and in the solid state by X-ray crystallography. Complex 3 was tested in vitro against a number of cell lines. For example, it inhibited K562 leukaemia cells with an IC(50) value of 4.3 microM (1 h exposure) and displayed cathepsin B inhibitory action with an IC(50) value of 3 microM.
|Additional Information:|| This paper is published as part of a Dalton Transactions themed issue on Bioorganometallic Chemistry, with Guest Editor, Charles Riordan,University of Delaware, USA (Number 22, 14 June 2009).|
|Uncontrolled Keywords:||organometallic chemistry, antitumor-activity, complexes, drugs, precatalysts, inhibitors, palladium, design, agents|
|Subjects:||Q Science > QD Chemistry|
R Medicine > RS Pharmacy and materia medica
|School / Department / Research Groups:||School of Science|
School of Science > Department of Pharmaceutical, Chemical & Environmental Sciences
|Last Modified:||29 Mar 2012 11:06|
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