120339-19-7Relevant academic research and scientific papers
Nonsteroidal Anti-inflammatory-Organometallic Anticancer Compounds
P?unescu, Emilia,McArthur, Sarah,Soudani, Mylène,Scopelliti, Rosario,Dyson, Paul J.
, p. 1788 - 1808 (2016)
Compounds that combine metal-based drugs with covalently linked targeted organic agents have been shown, in some instances, to exhibit superior anticancer properties compared to the individual counterparts. Within this framework, we prepared a series of organometallic ruthenium(II)- and osmium(II)-p-cymene complexes modified with the nonsteroidal anti-inflammatory drugs (NSAIDs) indomethacin and diclofenac. The NSAIDs are attached to the organometallic moieties via monodentate (pyridine/phosphine) or bidentate (bipyridine) ligands, affording piano-stool Ru(II) and Os(II) arene complexes of general formula [M(n6-p-cymene)Cl2(N)], where N is a pyridine-based ligand, {2-(2-(1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl)acetoxy)ethyl-3-(pyridin-3-yl)propanoate} or {2-(2-(2-((2,6-dichlorophenyl)amino)phenyl)acetoxy)ethyl-3-(pyridin-3-yl)propanoate}, [M(n6-p-cymene)Cl2(P)], where P is a phosphine ligand, {2-(2-(1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl)acetoxy)ethyl-4-(diphenylphosphanyl)benzoate} or {2-(2-(2-((2,6-dichlorophenyl)amino)phenyl)acetoxy)ethyl-4-(diphenylphosphanyl)benzoate, and [M(n6-p-cymene)Cl(N,N′)][Cl], where N,N′ is a bipyridine-based ligand, (4′-methyl-[2,2′-bipyridin]-4-yl)methyl-2-(1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl)acetate), (4′-methyl-[2,2′-bipyridin]-4-yl)methyl-2-(2-((2,6-dichlorophenyl)amino)phenyl)acetate), (bis(2-(2-(1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl)acetoxy)ethyl)[2,2′-bipyridine]-5,5′-dicarboxylate), or (bis(2-(2-(2-((2,6-dichlorophenyl)amino)phenyl)acetoxy)ethyl)[2,2′-bipyridine]-5,5′-dicarboxylate). The antiproliferative properties of the complexes were assessed in human ovarian cancer cells (A2780 and A2780cisR, the latter being resistant to cisplatin) and nontumorigenic human embryonic kidney (HEK-293) cells. Some of the complexes are considerably more cytotoxic than the original drugs and also display significant cancer cell selectivity.
Synthesis of furoxan derivatives of diclofenac as potent anti-inflammatory agents with reduced GI toxicity
Amir, Mohd,Akhter, Md. Wasim,Somakala
, p. 989 - 998 (2017/11/10)
A new series of NO donating furoxan derivatives of diclofenac have been synthesized by linking diclofenac to selected furoxan moieties and have been investigated for their anti-inflammatory, analgesic, ulcerogenic, lipid peroxidation, hepatotoxicity, histopathological and NO releasing properties. All the hybrid derivatives are endowed 'with antiinflammatory activity comparable to diclofenac but unlike this drug they show reduced GI toxicity. The compounds 4-[(2-(2-(2-(2,6-dichlorophenylamino)phenyl)acetamido)ethoxy)carbonyl]-3-methyl furoxan 12 having amide-ester linkage and 4-[(2-(2-(2,6-dichlorophenylamino)phenyl)acetoxy)methyl]-3-methyl-furoxan 13a having ester linkage show greater anti-inflammatory activity comparable to standard drug diclofenac. These compounds 12 and 13a also show higher gastrointestinal protection in comparison to standard drug diclofenac.
N-PHENYL ANTHRANILIC ACID DERIVATIVES AND USES THEREOF
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Page/Page column 45, (2009/04/25)
ABSTRACT Compounds that can be used as openers or blockers of voltage-dependent potassium channels, and which are useful in the treatment of conditions such as central or peripheral nervous system disorders through the modulation of potassium ion flux thr
