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The condensation of alkylenediamines with quinizarin or with 2,3-dihydro-1,4,5,8-tetrahydroxy-9,10-anthracenedione, followed by oxidation, gave 1,4-bis[aminoalkyl)amino]-9,10-anthracenediones. Some of these compounds and their 2,3-dihydro derivatives were markedly active against both leukemias and solid tumors in mice. Activity was maximal with… (More)
OBJECTIVES Gastroesophageal reflux disease (GERD) and irritable bowel syndrome (IBS) are highly prevalent in the general population, with significant symptom overlap, whereas the interaction between both remains poorly understood. We aim to identify the clinical and psychological factors that contribute toward the overlap of GERD and IBS. PATIENTS AND… (More)
OBJECTIVE Acute administration of 5-hydroxytryptamine4 (5-HT4) receptor agonist, mosapride or esophageal infusion of the transient receptor potential vanilloid receptor-1 (TRPV1) agonist capsaicin promotes secondary peristalsis. We aimed to investigate whether acute esophageal instillation of capsaicin-containing red pepper sauce or administration of… (More)
By using inhibition of histamine release from antigen-challenged, sensitized human basophils as a means of identifying a potentially prophylactic drug for the treatment of asthma, a series of substituted imidazo[1,5-d][1,2,4]triazines were found, which were active. These compounds were prepared by treating imidazolecarboxaldehydes with excess Grignard agent… (More)
A series of 3,6-bis(aminoalkoxy)acridines (2) was prepared and shown to have a protective antiviral effect against an interferon-sensitive virus (Columbia SK) and to partially restore an antibody response to a T-cell-dependent antigen in leukemic immunosuppressed mice. The presence of circulating interferon and the stimulation of natural killer cell… (More)
9,10-Anthracenedicarboxaldehyde bis[(4,5-dihydro-1H-imidazol-2-yl)hydrazone] (bisantrene, VI-1) showed anticancer activity in mice vs. both leukemias and solid tumors. Increases in life span vs. the following neoplasms were: P-388 leukemia, 137%; B-16 melanoma, 122%; Lieberman plasma cell tumor, greater than 85%; colon tumor 26, 150%; Ridgway osteogenic… (More)
Bisamidines of 2,6-diaminoanthraquinone have demonstrated potent activity against cecal and hepaticEntamoeba histolytica infections in rats and hamsters, respectively. A number of these compounds compared favorably, in overall drug efficacy, with metronidazole and other standard agents.
The preparation and biological activities of a series of pyrido[3,4-e]-1,2,4-triazines, 1,2,4-triazino[5,6-c]quinolines, and related fused triazines are described. Methyl, amino, and acylamino substituents were placed in the pyridyl ring of the former system. Other structural modifications included various alkyl, cycloalkyl, substituted phenyl, and… (More)
A series of bisamidines of 2,6-diaminoanthraquinone was synthesized and tested against cecal and hepatic forms of Entamoeba histolytica infections in rats and hamsters, respectively. A number of compounds were found to have good activity against infections in both species.
A series of amidines and sulfonamides of 5- and 6-amino-2,3-bis(4-alkyl-1-piperazinyl)quinoxalines was synthesized and tested against cecal and hepatic forms of Entamoeba histolytica infections in rats and hamsters, respectively. Four compounds (5, 6, 8, and 9) were found to have acceptable activity against infections in both species but were too toxic to… (More)