Refernces
10.1021/ja5038269
The study presents the development of a series of platinum(IV) prodrugs, specifically designed to enhance interaction with human serum albumin (HSA) for drug delivery purposes. The prodrugs were synthesized by asymmetrically functionalizing the axial ligands to mimic the features of a fatty acid, with the aim of improving cellular uptake and cytotoxicity. The lead compound, 4e, which has a hexadecyl chain, demonstrated a significant therapeutic potential due to its ability to form a tight, non-covalent complex with HSA (complex 7), enhancing its stability in blood and reducing the rate of reduction by ascorbate. The study involved platinum(IV) complexes with varying aliphatic tail lengths, including 4a, 4b, 4c, 4d, and 4e, which were used to investigate the impact of lipophilicity on cellular uptake and cytotoxicity. Other chemicals used included cisplatin as a reference compound, succinic anhydride, isocyanate reagents for the synthesis of the prodrugs, and ascorbate as a biological reductant to study the reduction of the Pt(IV) prodrugs. The purpose of these chemicals was to create a novel class of anticancer prodrugs with improved properties, such as enhanced stability, reduced side effects, and potentially increased efficacy.
10.1039/c9ob00900k
The study investigates the factors influencing the distribution behavior of cytochrome c (cyt.c) in a biphasic system composed of tetrabutylphosphonium 2,4,6-trimethylbenzenesulfonate ([P4,4,4,4][TMBS]) and potassium phosphate buffer (PKB). The researchers modified the surface of cyt.c using three different chemicals: acetic anhydride for acetylation, succinic anhydride for succinylation, and N-hydroxysuccinimide activated triethylene glycols (TEGs) with varying terminal alkyl chain lengths (methyl, ethyl, and butyl) to alter its surface charge and hydrophobicity. Acetylation resulted in the loss of a positive charge, succinylation exchanged a positive charge to a negative charge, and TEG modification added an amphipathic unit. The study found that the distribution ratio of cyt.c into the [P4,4,4,4][TMBS] phase decreased with decreasing isoelectric point (pI) of the protein. Additionally, at low pI values (around 4), the surface hydrophobicity of the modified cyt.c, influenced by the type of TEG modifier, significantly affected its distribution behavior. The findings suggest that both the pI and surface hydrophobicity of cyt.c are crucial factors controlling its distribution in the biphasic system, providing insights for protein separation and recycling in temperature-sensitive aqueous and non-aqueous biphasic systems.
10.1021/ol016093m
2'-Deoxy-5'-O-(4,4'-dimethoxytrityl)uridine (1) is a protected nucleoside, specifically a protected deoxyuridine. The 5'-hydroxyl group is protected with a 4,4'-dimethoxytrityl (DMT) group, which is commonly used in solid phase oligonucleotide synthesis to prevent unwanted reactions at the 5' position. It serves as a starting material for the synthesis of nucleoside phosphoramidite building blocks. The DMT group can be removed later in the synthesis to allow for further functionalization. 2-Cyanoethyl N,N,N',N'-tetraisopropylphosphoramidite is a phosphoramidite reagent used in the phosphorylation step of nucleoside phosphoramidite synthesis. It is used to convert nucleoside derivatives (2a-d) into the desired phosphoramidites (3a-d) which are then used in machine-assisted DNA synthesis. Succinic anhydride, a cyclic anhydride used for alcohol esterification, was used to convert the nucleoside derivative 2a to the corresponding succinate ester (17), which was then immobilized on a long-chain alkylamine CPG polymer support.
10.1248/cpb.31.4001
The research focuses on the development of immunoassays for tetrahydro-11-deoxycortisol (THS) and its glucuronides. Various haptenic derivatives, including the 3-hemisuccinate (15), 21-hemisuccinate (8), 3-hemiglutarate (16), 21-hemiglutarate (9), and glucuronides (19, 23, 25) of THS, were synthesized starting from 11-deoxycortisol 21-acetate (1). These derivatives were used to produce anti-THS 3-glucuronide antisera in rabbits and to prepare enzyme-labeled antigens for immunoassays. The antisera demonstrated binding affinities to the enzyme-labeled antigens, and the binding was inhibited by the glucuronide (19) in the enzyme immunoassay procedure. Key chemicals involved in the research include 11-deoxycortisol 21-acetate, succinic anhydride, glutaric anhydride, tert-butyldimethylsilyl chloride, and various reagents for the Koenigs-Knorr reaction, such as silver carbonate and methyl 1-bromo-1-deoxy-2,3,4-tri-O-acetyl-α-D-glucopyranuronate.
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