alexa Synthesis of Novel Palladacycles Inhibitors of the Cathepsin B Activity and Antitumoral Agents | OMICS International | Abstract
ISSN: 2161-0444

Medicinal Chemistry
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Research Article

Synthesis of Novel Palladacycles Inhibitors of the Cathepsin B Activity and Antitumoral Agents

Abdel-Sattar S Hamad Elgazwy1*, Mohamed R Shehata2, Myssoune Y Zaki3, Dalia H S Solima4 and Marwa M Elbakkry1,2

1Department of Chemistry, Faculty of Science, Ain Shams University, Abbassia 11566, Cairo, Egypt

2Department of Chemistry, Faculty of Science, Cairo University, Giza, Egypt

3National Organization for Drug Control and Research, Cairo, Egypt

4Department of Pharmaceutical Chemistry, Faculty of Pharmacy (Girls' Branch), Al Azahar University, Nasser city, Cairo, Egypt

*Corresponding Author:
Abdel-Sattar S Hamad Elgazwy
Department of Chemistry, Faculty of Science
Ain Shams University, Abbassia 11566, Cairo, Egypt
Tel/Fax: 002024831836
E-mail: [email protected]

Received date: July 22, 2013; Accepted date: August 29, 2013; Published date: August 30, 2013

Citation: Hamad Elgazwy ASS, Shehata MR, Zaki MY, Solima DHS, Elbakkry MM (2013) Synthesis of Novel Palladacycles Inhibitors of the Cathepsin B Activity and Antitumoral Agents. Med chem 3:254-261. doi:10.4172/2161-0444.1000148

Copyright: © 2013 Hamad Elgazwy ASS, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

Abstract

The reaction of 2-bromo-3,4,5-trimethoxybenzaldehyde 1 with Pd(dba) 2 ; dba=dibenzylideneacetone) in the presence of a stoichiometric amount of nitrogen donor ligands, such as N,N,N’,N’ -tetramethyl-ethane-1,2-diamine (TMEDA), 2,2’-bipyridine (bpy) 4,4’-dimethyl-2,2’-bipyridine (dmbpy) and an 1,10-phenanthroline (Phen), should be added to with equimolar ratio in degassed acetoneunder nitrogen to give mononuclear σ-aryl palladium (II) complexes cis-[2- Pd{C 6 H(CHO)-6-(OMe) 3 -3,4,5}BrL 2 ] 3a-d, where L 2 =TMEDA (3a); L 2 =bpy (3b); L 2 =dmbpy (3c); L 2 =Phen (3d) in good yields 48-65%. The reaction of the synthesized five-membered C,N -palladacycle cis-[2-Pd{C 6 H(CHO)-6-(OMe) 3 -3,4,5} BrL 2 ] 3a-d, where L 2 =TMEDA (3a); L=bpy (3b); L 2 =dmbpy (3c); L 2 =Phen (3d), with an1-naphthylisocyanates (C 10 H 7 - NCO) and an 1-naphthylisothiocyanates (C 10 H 7 -NCS), leads to the formation of novel palladacycle 4a-d and 5a-d, which was characterized in solution by 1 H NMR spectroscopy. The solid products were characterized by satisfactory elemental analysis and spectra studies. All the resulting complexes 3a-d, 4a-d and 5a-d were tested in vitro against a number of cell lines. For example, it inhibited K562 leukaemia cells with an IC 50 value in the range of (3.00 -4.3) μM (1 h exposure) and displayed cathepsin B inhibitory action with an IC 50 value in the range of (0.045-0.055 μM)

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