Synthesis of a 1,4-benzodiazepine containing palladacycle with in vitro anticancer and cathepsin B activity
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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)
Full text not available from this repository.Abstract
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.
| Item Type: | Article |
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| Additional Information: | [1] 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 |
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| Last Modified: | 29 Mar 2012 11:06 |
| URI: | http://gala.gre.ac.uk/id/eprint/1602 |
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