ICRF-193
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ICRF-193
ICRF 193 is a topoisomerase inhibitor Topoisomerase inhibitors are chemical compounds that block the action of topoisomerases, which are broken into two broad subtypes: type I topoisomerases (TopI) and type II topoisomerases (TopII). Topoisomerase plays important roles in cellular rep .... References Imides Diketopiperazines Topoisomerase inhibitors {{organic-compound-stub ...
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Topoisomerase Inhibitor
Topoisomerase inhibitors are chemical compounds that block the action of topoisomerases, which are broken into two broad subtypes: type I topoisomerases (TopI) and type II topoisomerases (TopII). Topoisomerase plays important roles in cellular reproduction and DNA organization, as they mediate the cleavage of single and double stranded DNA to relax supercoils, untangle catenanes, and condense chromosomes in eukaryotic cells. Topoisomerase inhibitors influence these essential cellular processes. Some topoisomerase inhibitors prevent topoisomerases from performing DNA strand breaks while others, deemed topoisomerase poisons, associate with topoisomerase-DNA complexes and prevent the re-ligation step of the topoisomerase mechanism. These topoisomerase-DNA-inhibitor complexes are cytotoxic agents, as the un-repaired single- and double stranded DNA breaks they cause can lead to apoptosis and cell death. Because of this ability to induce apoptosis, topoisomerase inhibitors have gained int ...
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Imides
In organic chemistry, an imide is a functional group consisting of two acyl groups bound to nitrogen. The compounds are structurally related to acid anhydrides, although imides are more resistant to hydrolysis. In terms of commercial applications, imides are best known as components of high-strength polymers, called polyimides. Inorganic imides are also known as solid state or gaseous compounds, and the imido group (=NH) can also act as a ligand. Nomenclature Most imides are cyclic compounds derived from dicarboxylic acids, and their names reflect the parent acid. Examples are succinimide, derived from succinic acid, and phthalimide, derived from phthalic acid. For imides derived from amines (as opposed to ammonia), the ''N''-substituent is indicated by a prefix. For example, N-ethylsuccinimide is derived from succinic acid and ethylamine. Isoimides are isomeric with normal imides and have the formula RC(O)OC(NR′)R″. They are often intermediates that convert to the more symmet ...
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Diketopiperazines
A diketopiperazine (DKP), also known as a ''dioxopiperazine'' or ''piperazinedione'', is a class of organic compounds related to piperazine but containing two amide linkages. DKP's are the smallest known class of cyclic peptide. Despite their name, they are not ketones, but amides. Three regioisomers are possible, differing in the locations of the carbonyl groups. * One isomer is an oxamide obtained from ethylenediamine. * 2,5-Diketopiperazines are cyclodipeptides often obtainable via condensation of two α- amino acids. * 2,6-Diketopiperazines may be viewed as cyclized imide derivatives derived from iminodiacetic acids. Of these three isomeric diketopiperazines, the 2,5-derivatives have attracted the greatest interest. Due to their appearance in biologically active natural products, medicinal chemists have been inspired to use DKPs to circumvent the poor physical and metabolic properties of peptides in the course of drug discovery. Natural sources DKPs are synthesized ...
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