Density, Speed of Sound, Viscosity, and Excess Properties of <i>N</i>‑Ethyl-2-pyrrolidone + 2‑(Methylamino)ethanol [or 2‑(Ethylamino)ethanol] from <i>T</i> = (293.15 to 323.15) K

Density, speed of sound, and viscosity of the binary mixtures <i>N</i>-ethyl-2-pyrrolidone (EP) + 2-(methylamino)­ethanol [or 2-(ethylamino)­ethanol] were measured at different temperatures from (293.15 to 323.15) K and over the entire range of concentrations. The excess isentropic compressibility, excess molar volumes, and viscosity deviations were calculated. Beside, the excess molar volumes were fitted using a Redlich–Kister equation, and the viscosity data were fitted by the Grunberg–Nissan model

Synthesis and Biological Evaluation of 1α,25-Dihydroxyvitamin D₃ Analogues with a Long Side Chain at C12 and Short C17 Side Chains

Structure-guided optimization was used to design new analogues of 1α,25-dihydroxyvitamin D₃ bearing the main side chain at C12 and a shorter second hydroxylated chain at C17. The new compounds <b>5a</b>–<b>c</b> were efficiently synthesized from ketone <b>9</b> (which is readily accessible from the Inhoffen–Lythgoe diol) with overall yields of 15%, 6%, and 3% for <b>5a</b>, <b>5b</b>, and <b>5c</b>, respectively. The triene system was introduced by the Pd-catalyzed tandem cyclization–Suzuki coupling method. The new analogues were assayed against human colon and breast cancer cell lines and in mice. All new vitamin D₃ analogues bound less strongly to the VDR than 1α,25-dihydroxyvitamin D₃ but had similar antiproliferative, pro-differentiating, and transcriptional activity as the native hormone. In vivo, the three analogues had markedly low calcemic effects