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Palladium (II) complexes containing n-heterocyclic carbene ligand, synthesis, and applications in cancer treatment

A technology of heterocyclic carbene and complexes, applied in the field of palladium (II) complexes containing N-heterocyclic carbene ligands, synthesis, and application in cancer treatment, capable of solving undesired high reactivity substitution reactions, Low in vivo stability and multiple forms, complex therapeutic applications and other issues

Active Publication Date: 2019-05-24
THE UNIVERSITY OF HONG KONG
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, only a few palladium(II) complexes exhibit good anticancer activity in vivo
The main challenges in developing anticancer palladium(II) complexes are their undesirably high reactivity towards sulfur-containing biomolecules such as glutathione (GSH) and their susceptibility to substitution reactions under physiological conditions, resulting in low in vivo stability and multiple morphology, which complicates potential therapeutic applications

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  • Palladium (II) complexes containing n-heterocyclic carbene ligand, synthesis, and applications in cancer treatment
  • Palladium (II) complexes containing n-heterocyclic carbene ligand, synthesis, and applications in cancer treatment
  • Palladium (II) complexes containing n-heterocyclic carbene ligand, synthesis, and applications in cancer treatment

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[0031] Terms not specifically defined herein shall be given meanings given by those skilled in the art according to the present disclosure and the context. However, as used in this specification, unless stated to the contrary, the following terms have the indicated meanings and are subject to the following conventions.

[0032] It is to be understood that, unless otherwise stated, this invention is not limited to particular reactants, reaction conditions, etc., as these may vary. It is also to be understood that terminology used herein is for the purpose of describing particular embodiments only and is not intended to be limiting.

[0033] As used in the specification and the appended claims, the singular forms "a," "an," and "the" include plural referents unless the context clearly dictates otherwise. Thus, for example, reference to "a catalyst" or "a complex" includes combinations or mixtures of different catalysts or complexes as well as a single catalyst or complex, and r...

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Abstract

Palladium (II) N-heterocyclic carbene (NHC) complexes which are stable in the presence of biological thiols. A representative complex, [Pd (C^N^N) (N, N' -nBu 2NHC) ] (CF 3SO 3) (Pd1d, HC^N^N= 6-phenyl-2, 2 ' -bipyridine, N, N'-nBu 2NHC=N, N'-di-n-butylimidazolium), displays potent killing activity toward cancer cell lines but is less cytotoxic toward normal human fibroblast cell lines.

Description

technical field [0001] Here we describe palladium(II) N-heterocyclic carbene (NHC) complexes stabilized in the presence of biothiols that exhibit potent killing activity against cancer cell lines. Background of the invention [0002] In addition to catalysis, there is growing interest in extending the range of applications of palladium complexes, such as functional molecular materials and organic electronics. In this regard, palladium(II) complexes have recently been investigated as potential anticancer chemotherapeutic agents. The antiproliferative properties of palladium complexes have been reported since the 1980s. Most of the reported palladium(II) complexes show some DNA binding properties. However, only a few palladium(II) complexes exhibit good anticancer activity in vivo. The main challenges in developing anticancer palladium(II) complexes are their undesirably high reactivity towards sulfur-containing biomolecules such as glutathione (GSH) and their susceptibilit...

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F17/02C07F17/00A61K31/435A61K31/41A61K31/015A61P35/00
CPCA61K31/4178A61K31/444A61K31/4725A61K31/66A61K31/7135A61P35/00
Inventor 支志明方祉谦陆振南周沛强
Owner THE UNIVERSITY OF HONG KONG
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