Breast cancer resistance protein (BCRP, ABCG2) is a recently identified member of the ATP-binding cassette family of cell surface transport proteins. This study was conducted to investigate the effect of a series of newly synthesized 1,4-dihydropyridines and pyridines, designed as potent P-glycoprotein inhibitors, on BCRP-mediated drug efflux both in vitro and in vivo. The effects of 25 synthes...

A variety of Hantzsch 1,4-dihydropyridines were oxidized to their corresponding pyridines in high yields in the presence of Cu(C22H22N2O2) in refluxing acetic acid.

2-monobromomethyl 1,4-dihydropyridines is selectively synthesized by bromination of the parent compound by 1.1 equivalents of pyridinium bromide perbromide in dichloromethane/pyridine at -20 °C. The same reagent in dichloromethane at 0 °C produce the 2,6-bis(bromomethyl) 1,4-dihydropyridines.

The reactions of sec-aminodienyl esters 3 with crotonaldehyde (4) afforded N-alkyl 3-[2-(methoxycarbonyl)ethenyl]-4-methyl-1,4-dihydropyridines 5, providing a new azaelectrocyclization reaction.

in this study, oxidation of some 3,5-diacyl or 3,5-diester 1,4-dihydropyridines to corresponding pyridine derivatives using sodium bromate in the presence of nh4cl, nahso4 and bu4nhso4 under thermal conditions has been investigated. the yield and structure of formed products is similar under all conditions; however, the reaction is accelerated in the presence of bu4nhso4 and nahso4. in addition...

The calmodulin inhibitors R24571 and trifluoperazine were found to inhibit competitively the binding of [3H]nitrendipine to a 48,000 X g particulate fraction of rat brain with IC50 values of 1.0 and 18.8 microM, respectively. Equilibrium dialysis was used to test the ability of the dihydropyridines nitrendipine, felodipine, and nicardipine to inhibit the binding of [3H]chlorpromazine, [14C]pimo...

The kinetic features of the interaction of dihydropyridines with rat aortic smooth muscle were investigated in parallel mechanical and binding studies. The inhibitory action of (+)-PN200-110 and nisoldipine on contractions evoked by potassium chloride depolarization was characterized by a pronounced time dependency, in which the inhibition increased slowly after depolarization to attain a stead...

Voltage-dependent calcium channels play a role in many cellular phenomena. Very little is known about Ca2+ channels in Drosophila, especially those in muscles. Existing literature on neuronal Ca2+ channels of Drosophila suggests that their pharmacology may be distinct from that of vertebrate Ca2+ channels. This raises questions on the pharmacology and diversity of Ca2+ channels in Drosophila mu...

The reaction of a sec-nitrodienamine 3 with aldehyde compounds afforded 2-substituted 3-nitro-1,2-dihydropyridines 5, providing a heterocyclic annulation reaction.

In this study, oxidation of some 3,5-diacyl or 3,5-diester 1,4-dihydropyridines to corresponding pyridine derivatives using sodium bromate in the presence of NH4Cl, NaHSO4 and Bu4NHSO4 under thermal conditions has been investigated. The yield and structure of formed products is similar under all conditions; however, the reaction is accelerated in the presence of Bu4NHSO4 and NaHSO4. In addition...