1,721,029 research outputs found
Synthesis, molecular modeling and biological evaluation of fullerene-trimethoxyindole-oligonucleotide conjugates: a possible probe for studing photochemical reactions in DNA triple helices.
No full textOligonucleotides and oligonucleotide conjugates: A new approach for cancer treatment
No full textIn this account we summarise recent studies on oligonucleotides and
oligonucleotide derivatives and their utilisation in antigene, antisense and
decoy approaches, with particular attention to peptide nucleic acids, locked
nucleic acids and oligonucleotide conjugates, the most promising compounds in
this field
Synthesis and structural characterization of single-walled carbon nanotubes functionalized with fluorinated phosphonate analogues of phenylglycine, as promising materials for synthetic and biomedical applications
No full textThrough chemical functionalization the prerequisites for possible applications of such nanostructures as single-walled carbon nanotubes (SWCNTs) are established. In this study, modifications of SWCNTs by fluorinated phosphonate analogue of phenylglycine, compound belonging to important group of natural amino acid mimetics, using two approaches are presented. The first one was based on noncovalent functionalization of SWCNTs with the phosphono-perfluorophenylglycine analogue. In the second approach, SWCNTs were covalently bonded to the fluorinated α-aminophosphonates in one-step or multi-step reactions. The investigation of the functionalization effect on the dispersibility, thermal properties and the structure of SWCNTs was performed by using of X-Ray spectroscopy, TGA and Raman spectroscopy. Both approaches indicated promising methods for fast and efficient modification of carbon nanotubes (CNTs) also with other representatives of previously synthesized fluorinated aminophosphonates. Functionalized with such compounds CNTs can constitute materials for synthetic and biomedical applications. Due to their biological activity and structural analogy to corresponding α-amino acids, fluorinated α-aminophosphonates provide an important source for drug discovery. Therefore functionalization of SWCNTs with such molecules can provide an important platforms for drug delivery applications. Due to the presence of perfluorinated phenyl rings various nucleophiles can be introduced by nucleophilic aromatic substitution reactions to the functionalized SWCNTs leading to obtaining completely new materials
CC-1065 and the duocarmycins: recent developments
No full textIt is accepted that neoplastic diseases are related to gene alteration or oncogene activation. In particular, DNA minor groove binding drugs have been extensively studied through the years in order to influence the regulation of gene expression by means of specific interactions with DNA based moieties. In this field, analogues of naturally occurring antitumour agents, such as CC-1065 and/or the duocarmycins, represent a new class of highly potent antineoplastic compounds, currently under investigation. CC-1065 and duocarmycins represent a class of exceptionally potent antitumour antibiotics that derive their biological effects from the reversible, stereo-electronically-controlled sequence selective alkylation of DNA. All natural compounds showed a cytotoxicity against leukaemia L1210 cell lines in the range 10-220pM but while CC-1065 showed a good antitumour activity in an in vivo model (optimal dose from 10-100 μg/g), duocarmycins showed weak antitumour activity. Despite its potency, CC-1065 cannot be used in humans due to eventual fatality. For this reason many scientists have focused their attention on this class of compounds, in order to obtain new derivatives with equal in vitro potency but a better profile in in vivo models. This effect is accompanied by dramatic changes in the morphology of hepatic mitochondria. On this basis, the recent developments on SARs for this class of compounds and their possible use as therapeutic agents are reviewed, with particular emphasis on recent patent literature and, finally, a conclusive opinion will be given on this topic
Design and Synthesis of Novel [60]Fullerene Derivatives as Potential HIV Aspartic Protease Inhibitors.
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