Read Structure-Activity Studies of Polyamine Analogues as Antineoplastics (Classic Reprint) - Yang Feng file in PDF
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Herein, we describe a series of structure–activity relationship studies that provide an enhanced understanding of the effectiveness of certain cyclopropenimines as enantioselective brønsted base catalysts. These studies underscore the crucial importance of dicyclohexylamino substituents in mediating both reaction rate and enantioselectivity.
Fourteen polyamine analogues, asymmetric or symmetric substituted spermine (1-9) or methoctramine (10-14) analogues, were evaluated as potential inhibitors or substrates of two enzymes of the polyamine catabolic pathway, spermine oxidase (smox) and acetylpolyamine oxidase (paox).
A phase i study of a new polyamine biosynthesis inhibitor, sam486a, in cancer patients with solid tumours.
The studies clearly indicate that polyamine length, charge, and terminal nitrogen substitution have a significant effect on how the tetraamine regulates mk-801 binding to the nmda receptor. Thus a structure-activity basis set on which future design of mk-801 agonists and antagonists can be based is now available.
As a part of our continuing studies on 'polyamines and their role in human disease' our considerations of structure–activity relationships (sar) within naturally.
The lamellarins exhibit broad anticancer activity [8,9], and the majority of structure-activity relationship (sar) studies indicated that they are multi-target anticancer agents, for instance, they have topo i inhibition activity [10,11], mitochondrial apoptotic activity [, ], reversal of multidrug resistance activity [15,16], and kinase.
Thus, this systematic sar study has provided new pharmacological tools for studies of iglu receptors.
2008, 51, 7308–7312 structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone.
Increased synthesis of adomet but not of methionine during testosterone stimulation of polyamine studies on the oxidation state and biosynthesis of molybdopterin effect of limited proteolysis on structure and activity of phenylal.
Structure-activity studies showed a clear dependence of the acyl chain length on activity against lta in compounds with spermine and homospermine scaffolds.
We also include the recent structure–activity relationship studies and application of polyamine toxins as biological tools, including developing selective iglu subtype receptors and nach.
Structure-activity studies of polyamine analogues as antineoplastics item preview remove-circle share or embed this item.
This structure-activity set makes it possible to establish the importance of charge, intercharge distance, and terminal nitrogen substitution on polyamine-regulated mk-801 binding in the nmda.
Structure-activity investigations of polyamine-anthracene conjugates and their uptake via the polyamine transporter summary. A series of polyamine conjugates were synthesized and evaluated for their ability to target the polyamine abbreviations.
15 jan 2002 several studies have shown the association of polyamines to dna to of polyamines under conditions of low water activity (18) and possibly.
This structure−activity set makes it possible to establish the importance of charge, intercharge distance, and terminal nitrogen substitution on polyamine-regulated mk-801 binding in the nmda channel. Four families of tetraamines are included in this set: norspermines, spermines, homospermines, and tetraazaoctadecanes.
The diversity of biological research in the polyamine field is the subject of an ( 1994) antiproliferative properties of polyamine analogues: a structure-activity.
The critical role of polyamines in cell growth has led to the development of a number of agents that interfere with polyamine metabolism. Polyamine analogues upregulate p53 in a cell leading to restriction of proliferation and apoptosis.
We and others have performed extensive structure–activity relationship (sar) studies of polyamine toxins as iglu receptor ligands, 7 initially using the wasp polyamine toxin, philanthotoxin‐433, as a template. 9 more recently, we have used the structurally more complex and more potent spider polyamine toxins, such as argiotoxin‐636 (argtx‐636), 7d 10 as a template for developing polyamine toxin derivatives with an improved selectivity profile.
Studies with transgenic cancer models also support the finding that the effect of myc on tumor initiation and progression can be attenuated through the repression of polyamine production. High-risk neuroblastomas (an often lethal embryonal tumor in which myc activation is paramount) deregulate numerous polyamine enzymes to promote the expansion.
In this section, structure–activity relationships of polyamine analogs were described in terms of symmetry, steric hindrance, and conformational restriction. In addition, a variety of mechanisms for cytotoxicity have been reported. This section also deals with the mechanisms of action that have been suggested with a more significance.
We have synthesized a series of new β-lactam-azide derivatives as orally active anti-tumor agents by targeting tubulin colchicine binding site and examined their structure activity relationship.
In the present study, we have used genetic code reprogramming to synthesise very high diversity focused libraries (10 12 compounds) based on cp2 and, through affinity screening, used these to delineate the structure activity relationship of cp2 binding to kdm4a.
Fibrogenic structure-activity study of the bleomycin molecule. In the present study the fibrogenic potential of intact bleomycins as well as their acetyldipeptide and terminal polyamine constituents have been assessed.
Or spermidine, yet display substantially different structure activity relationships for polyamines that inhibit human carbonic anhydrases, biomed research.
19 dec 2016 we studied the effect of branched-chain polyamines on the folding transition of polyamines induce a crosslinked meshwork structure in a giant dna an important role in maintaining genetic activities at high temperat.
Abstract: this review describes the recent developments in the field of polyamine toxins, with focus on structure activity relationship investigations, including studies of importance of the polyamine moiety for biological activity, photolabeling studies using polyamine toxins as templates, as well as use of solid phase methods for the synthesis of polyamine toxins. The review is mainly concerned with effects of polyamine toxins on nicotinic acetylcholine receptors and ionotropic glutamate.
15 dec 2009 the highly sensitive structure–activity relationships (sar's) that underlie and control polyamine function have been the target of intense research.
We also include the recent structure–activity relationship studies and application of polyamine toxins as biological tools, including developing selective iglu subtype receptors and nach receptors antagonists, as well as templates to develop labeled and fluorescent polyamine toxin probes.
This review describes the recent developments in the field of polyamine toxins, with focus on structure activity relationship investigations, including studies of importance of the polyamine moiety for biological activity, photolabeling studies using polyamine toxins as templates, as well as use of solid phase methods for the synthesis of polyamine toxins.
Polyamines are low molecular weight aliphatic polycations, highly charged and ubiquitously present in all living cells. Interest has been increasing during the last 30 years in the naturally abundant polyamines putrescine (diamine), spermidine (triamine) and spermine (tetramine), which were demonstrated to be involved in a large number of cellular processes.
10 oct 2018 research output: contribution to journal › article › peer-review fingerprint dive into the research topics of 'investigating structure property.
Finally, inclusion of reducible disulfide bonds to the polymer backbone increased transfection activity and reduced cytotoxicity.
Selective mammalian smo and pao inhibitors could represent important tools to study the involvement of this class of enzymes in polyamine homeostasis and in designing new antineoplastic drugs. Here, mpao and msmo inhibition by 1,8‐diaminooctane, 1,12‐diaminododecane, g3, guazatine and mdl72527 is reported.
The polyamine (pa) metabolism is involved in cell proliferation and differentiation. Increased cellular pa levels are observed in different types of cancers. These observations open a perspective to exploit the enzymes of pa catabolism as a target for anticancer drug design.
J med chem 44: 1–26 structure-activity studies of polyamine transport 313 marton lj, levin va, hervatin sj, koch-weser j, mccann pp, valasinas a, sarkar a, reddy vk, marton lj, basu hs, frydman b sjoerdsma a (1981) potentiation of the antitumor therapeutic effects (2001) conformationally restricted analogues of 1n,14n-bisethylho- of 1,3-bis(2-chloroethyl)-1-nitrosurea by alpha-difluoromethylornithine, mospermine (be-4-4-4): synthesis and growth inhibitory effects on an ornithine.
On the basis of our previous findings of effective hcc growth inhibition by the polyamine conjugates two hcc cell lines (hepg2, smmc7721) were selected for the in vitro screen of novel flavonoid-polyamine conjugates. Polyamines and/or flavonoids were assessed for selectivity between tumor and normal cells using one normal hepatocyte cell line (qsg7701).
These measurements included formal acute and chronic toxicity trials, drug and metabolic tissue distribution studies, and assessment of the impact of these analogues on tissue polyamine pools. Finally, the remarkable activity of n,n‘-bis[3-(ethylamino)propyl]-trans-1,4-cyclohexanediamine underscores the need to further explore this framework.
Mammalian polyamine catabolism is under the control of two enzymes, spermidine/spermine n 1-acetyltransferase and the flavin adenine dinucleotide-dependent polyamine oxidase (pao). In this study, the cloning and initial characterization of human pao is reported.
It is not clear how polyamine levels are affected in the course of healthy aging, since results across studies have been inconsistent, possibly because the studies looked at different brain areas. In one study, putrescine and spermine levels in occipital cortex were unaffected by age while spermidine levels.
Phanstiel o 4th, kaur n, delcros jg (2007) structure-activity investigations of polyamine-anthracene conjugates and their uptake via the polyamine transporter.
Polyamine research is a very active area with numerous publications covering genetic, biochemical and physiological studies using mammals, plants, protozoan parasites and many microorganisms, including thermophiles that have a wider variety of polyamines.
Recent studies indicate that induction of polyamine catabolic enzymes ssat and spermine oxidase (smo) play key roles in the anti-proliferative and apoptotic effects of polyamine analogues and their combinations with chemotherapeutic agents such as 5-fluorouracil (5-fu) and paclitaxel.
And the means by which polyamine content can be varied in response to exogenous stimuli are discussed. The role of polyamines in the cell cycle, cell division, tissue growth, and differentiation is considered. Recent studies using highly specific inhibitors of polyamine biosynthesis such as a-difluo-.
The evaluation of a group of polyamine analogs as agents to ameliorate the activity of the compounds is very dependent on both the nature of the in addition to the subcutaneous studies, several compounds, n1,n11- diethylnorspermin.
Amino acid residues) are actually considered as signal structures for the rapid and selective in the following experiments, therefore, the effects of putrescine were studied.
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