Optimization and kinetic model of condensation of a secondary amine with a uracil derivative in the synthesis of 2-[(1-carbethoxy-4-piperidinyl) (methyl)amino]-1H-pyrimidin-4-one.

A series of experiments was performed in order to determine the reaction conditions of 2-(methylsulfanyl)pyrimidin-4(3H)-one [U] with 4-(methylamino)piperidine [A] affording 2-[(1-carbethoxy-4-piperidinyl)(methyl)amino]-1H-pyrimidin-4-one [P] in a high yield (80%) (Scheme 1). Two theoretical approaches i.e.

Toxicity and antineoplastic effect of (24R)-1,24-dihydroxyvitamin D3 (PRI-2191).

Many efforts have been made to obtain active and less toxic Vitamin D analogs for new clinical applications. The results of previous studies demonstrated the efficacy and safety of topical treatment of psoriasis with one of these analogs, 1,24-dihydroxyvitamin D(3), tacalcitol (1,24-(OH)(2)D(3)). In the present study, we evaluated the toxicity and antitumor effect of this analog.

Synthesis and antiproliferative activity of side-chain unsaturated and homologated analogs of 1,25-dihydroxyvitamin D(2). (24E)-(1S)-24-Dehydro-24a-homo-1,25-dihydroxyergocalciferol and congeners.

A series of analogs of 1,25-dihydroxyergocalciferol (1-4) was synthesized and screened for their antiproliferative activity in vitro. The structure of new analogs was designed based on biological activity of the previously obtained side-chain modified analogs of vitamin D(2) and D(3). The analogs were obtained by the Julia olefination of C(22)-vitamin D sulfone 11 with side-chain aldehyde 15.