Measurement of natural environmental radioactivity and estimation of population exposure in Bihac,Bosnia and Herzegovina

Journal of Radioanalytical and Nuclear Chemistry - This work presents measurements of activity concentrations and estimation of population exposure from the naturally occurring radionuclides 238U,...     

Complete 1H and 13C assignments of fluorinated analogs of dehydroepiandrosterone

The complete assignments of all 1H and 13C chemical shifts were made for the fluorinated dehydroepiandrosterone (DHEA) analog fluasterone, 2, and two potential in vivo metabolites 3 and 4. The assignments were made using a combination of one- and two-dimensional NMR techniques (1H, 13C, gDQCOSY, gHSQC, gHMBC). Once the proton chemical shifts were assigned, the stereochemistry of the two hydroxylated analogs was determined using 2D ROESY experiments.     

Well‐Defined Polymer–Paclitaxel Prodrugs by a Grafting‐from‐Drug Approach

We report on the design of a polymeric prodrug of the anticancer agent paclitaxel (PTX) by a grafting‐from‐drug approach. A chain transfer agent for reversible addition fragmentation chain transfer (RAFT) polymerization was efficiently and regioselectively linked to the C2′ position of paclitaxel, which is crucial for its bioactivity. Subsequent RAFT polymerization of a hydrophilic monomer yielded well‐defined paclitaxel–polymer conjugates with high drug loading, water solubility, and stability. The versatility of this approach was further demonstrated by ω‐end post‐functionalization with a fluorescent tracer. In vitro experiments showed that these conjugates are readily taken up into endosomes where native PTX is efficiently cleaved off and then reaches its subcellular target. This was confirmed by the cytotoxicity profile of the conjugate, which matches those of commercial PTX formulations based on mere physical encapsulation.