Cancer is a leading cause of death worldwide. Despite the availability of several chemotherapeutic drugs, there is still a great need for more efficient agents for a better management of cancer. In this contribution, a series of 11 1,4-dihydropyridines (1,4-DHPs) (4a, 4b and 7a-i) were synthesized and evaluated for their cytotoxic effect against MCF-7, LS180 and MOLT-4 cancer cell lines using M...

The o-nitrophenyl group at position 4 of dihydropyridine of nifedipine analogues was replaced with 2-alkylthio-1-benzyl-5-imidazolyl substituent. Starting from dihydroxyacetone 2-alkythio-1-benzyl- 5-formyl imidazole (3) was first synthesized which was subsequently used in synthesizing symmetrical (5a-f) and asymmetrical (6a,b) dihydropyridines. Primarily pharmacological studies of the title co...

Abstract The antiprotozoal activity of 1-benzyltetrahydropyridin-4-yliden iminium salts is reported. This paper describes the preparation a series analogs from dihydropyridines or dihydrothiopyrans as educts. new compounds were investigated for their against Plasmodium falciparum NF54, causative organism Malaria tropica and Trypanosoma brucei rhodesiense , Human African Trypanosomiasis (sleepin...

Depolarization of NG108-15 (neuroblastoma-glioma) cells causes an increase in 45Ca2+ influx. This effect is blocked by low concentrations of dihydropyridines such as nitrendipine and by other blockers of voltage-sensitive calcium channels such as D-600, diltiazem, and Cd2+. Two other dihydropyridines, BAY K8644 and CGP 28392, have the opposite effect. Low concentrations of these compounds enhan...

Objective(s) Calcium-channel blockers have an important role in the treatment of several cardiovascular disorders. Derivatives of 1, 4-dihydropyridine are one of the most potent calcium antagonists. In this study four novel ', 4-dihydropyridine calcium channel blockers were synthesized and their hypotensive properties were investigated in male rats. Materials and Methods Four 1, 4-dihydropyr...

Reactions of 1 ,Zdihydropyridines (la-c) and 1,4-dihydropyridines (2a-c) in the presence of benzyne (3) under thermal conditions, and in the case of (2c) under photochemical conditions, have been investigated. Benzyne acts as an oxidizing agent to convert dihydropyridine (la) and (2a) to the corresponding pyridine (4) or adds as a dienophile to (lb-c).

The crucial role of L-type Ca2+ channels in the initiation of cardiac and smooth muscle contraction has made them major therapeutic targets for the treatment of cardiovascular disease. L-type channels share a common pharmacological profile, including high-affinity voltage- and frequency-dependent block by the phenylalkylamines, the benz(othi)azepines, and the dihydropyridines. These drugs are t...

Quantum chemical (MNDo)caleulations have beenused toelucidate the molecular properties and structure - activity relationships of dihydropyridine (DHP) type calcium antagonists. There is a good corielation between the net atomic charges on various atoms of the 4 - phenyl ring of dihydropyridines and pharmacological activity. .Also, activity decreases with increasing free rotation of the phen...