Artemisinin-Polypyrrole Conjugates: Synthesis, DNA Binding Studies and Preliminary Antiproliferative Evaluation was written by La Pensee, Louise;Sabbani, Sunil;Sharma, Raman;Bhamra, Inder;Shore, Emma;Chadwick, Amy E.;Berry, Neil G.;Firman, James;Araujo, Nuna C.;Cabral, Lilia;Cristiano, Maria L. S.;Bateman, Cerys;Janneh, Omar;Gavrila, Adelina;Wu, Yi Hang;Hussain, Afthab;Ward, Stephen A.;Stocks, Paul A.;Cosstick, Rick;O’Neill, Paul M.. And the article was included in ChemMedChem in 2013.Electric Literature of C10H12O3 This article mentions the following:
Seven artemisinin-polypyrrole conjugates were prepared Conjugate I emerges as the most active mol. being twofold more active than DHA against HT-29 cells and exhibiting around five times the potency of DHA against HL-60 cells. Conjugate I also exhibits one of the strongest affinities for the DNA duplex d(CGCGAATTCGCG). Structurally, these results are not surprising as conjugate I has the longest flexible linker, allowing for the greatest steric freedom to both portions of the hybrid. Modeling studies have accurately predicted the exptl. 铻朤m data, and decomposition of these calculated free energies of binding has shown that the binding affinity of these hybrid compounds depends on multiple factors, in particular electrostatic interactions and differential solvation of the ligand and DNA duplexes on complexation. Moreover, these factors are intrinsically linked to the varying degrees of conformational change the ligands and DNA duplex undergoes on binding. Further mechanistic studies are needed in HT-29 cells to clarify whether ART maintains mitochondrial membrane depolarization as a main mode of action or whether the presence of the DNA binding structure has in fact enhanced activity by causing a dual mode of action. In the experiment, the researchers used many compounds, for example, Methyl 2-(4-(hydroxymethyl)phenyl)acetate (cas: 155380-11-3Electric Literature of C10H12O3).
Methyl 2-(4-(hydroxymethyl)phenyl)acetate (cas: 155380-11-3) belongs to esters. Carboxylic acid esters of low molecular weight are colourless, volatile liquids with pleasant odours, slightly soluble in water. Acyl chlorides and acid anhydrides alcoholysis is another way to produce esters. Acyl chlorides and acid anhydrides react with alcohols to produce esters. Anydrous conditions are recommended since both acyl chlorides and acid anhydrides react with water.Electric Literature of C10H12O3
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics