2005
DOI: 10.2174/157018005774717299
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Anti-tumour Activity of Some Polydentate N-Ligands: N,N-bis-(3- Substituted-5-Methylpyrazol-1yl Methyl) Arylamines and N,N,N,N-Tetra- [(3-Substituted-5-Methylpyrazol-1yl] Para-Phenylenediamines

Abstract: Five polydentate ligands 2-6 were prepared from arylamines and precursors 1a-b . The polydentate (2-4) and (5) showed marked activity against cancer cell lines. The substituents (R and R') appear to play a key role in the cytotoxic potency of this class of compounds.

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Cited by 16 publications
(5 citation statements)
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“…Of the most important program, Osiris is already available online [33] and very useful for its design/prediction of various activities. In our recent publications [34,35,36,37,38,39,40,41,42,43] on the drug design of various pharmacophore sites by using spiro-heterocyclic structures, we have predicted activity and/or inhibition with increasing success in two targets, Mycobacterium tuberculosis and HIV. This is done by using a combined electronic/structure docking procedure.…”
Section: Resultsmentioning
confidence: 99%
“…Of the most important program, Osiris is already available online [33] and very useful for its design/prediction of various activities. In our recent publications [34,35,36,37,38,39,40,41,42,43] on the drug design of various pharmacophore sites by using spiro-heterocyclic structures, we have predicted activity and/or inhibition with increasing success in two targets, Mycobacterium tuberculosis and HIV. This is done by using a combined electronic/structure docking procedure.…”
Section: Resultsmentioning
confidence: 99%
“…Moreover, despite numerous reports on metal complexes with N-donor ligands [33,34], little is known regarding pyrazolyl-based late transition metal complexes as catalysts for methyl methacrylate polymerisation [35][36][37] compared with early transition metal complexes [38][39][40][41] because late transition metal complexes are generally more tolerant towards polar functional monomers (including MMA) due to their less-oxophilic nature. In contrast, the steric and electronic properties of pyrazolyl-based ligands can be fine-tuned by an appropriate choice of substitutions on the 2-N, 3-C, 4-C, and 5-C atoms of the pyrazole moiety [42][43][44][45], and have been employed in diverse potential applications [46][47][48][49][50]. In view of these promising features of pyrazolyl-based ligands, we focused on the synthesis, characterisation, and reactivity of various transition metal complexes with pyrazolyl-based ligands and their catalytic activities towards MMA polymerisation [18,51,52].…”
Section: Introductionmentioning
confidence: 99%
“…The range of pyrazoles enables optimization of the electrophilic properties of transition metal complexes of pyrazoles and their derivatives for use as catalysts for olefin polymerization. Thus, many pyrazoles and their transition metal complexes in different oxidation states have been isolated and structurally characterized, because of their diverse potential applications, including roles as industrial catalysts, such as in olefin oligomerization or polymerization [39,40], as bioinorganic materials in pharmaceutical preparations [41][42][43][44][45], and as metal ion extractants [46].…”
Section: Introductionmentioning
confidence: 99%
“…The range of pyrazoles enables optimization of the electrophilic properties of transition metal complexes of pyrazoles and their derivatives for use as catalysts for olefin polymerization. Thus, many pyrazoles and their transition metal complexes in different oxidation states have been isolated and structurally characterized, because of their diverse potential applications, including roles as industrial catalysts, such as in olefin oligomerization or polymerization [39,40], as bioinorganic materials in pharmaceutical preparations [41][42][43][44][45], and as metal ion extractants [46].These interesting features prompted us to explore the present system involving the N,N-bispyrazolylmethyl ligand, based on an aniline moiety [47,48] and their Co complexes to investigate the steric and electronic influence of substituents on the aniline ring in formation of complex and catalytic activity in both α-olefin and methyl methacrylate polymerization.Ligands [bpmaL1 -bpmaL4], were prepared in facile forms with high yields by dehydration of the alcoholic moiety of 1H-pyrazole-1-yl methanol,{R. Hüttel, 1952 #348} which readily undergoes sublimation, with aniline or substituted anilines, such as 2,6-diispropylaniline and 2,4,6-trimethylaniline. Solid ligands [bpmaL2-bpmaL4] and liquid ligand [bpmaL1] were very hydroscopic, with decomposition to the starting materials at certain time periods [49].…”
mentioning
confidence: 99%