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At least 19 recordsLinked to original sources
PubMed2002

Cancer chemotherapy and heterocyclic compounds.

The search for pharmacological approaches to neoplastic disease has made some impressive gains started after 1940 when the antileukemic activity of nitrogen mustard was discovered during world war II. It is generally accepted that neoplastic transformation is related to genes alteration or oncogene activation, so the progress in the development of the new drugs for treatment of malignant diseases has been rapid, both in revealing pathobiology of the diseases and discovery of new drugs. In addition attempts have been made to define optimal combinations, treatment strategies and patient support measures. Cancer chemotherapy is now of established value and a highly specialized field. Among the modifications to the family of antitumor compounds, heterocyclic organic compounds have been extensively applied by many groups in order to modify the reactivity profile. Pyrrole, pyrimidine, indole, quinoline and purine are few classes of heterocycles which showed interesting cytotoxicity profiles. The updated material related to these modifications has been rationalized and ordered, in order to offer an overview of the argument.

Animals↗
PubMed1991

[Monoamine oxidase inhibitory effects of pentanthrene type heterocyclic compounds].

Pentanthrene type heterocyclic compounds, which contain oxazole, isoxazole, oxadiazole, thiazole, isothiazole, thiadiazole or pyrrole ring as C-ring, and naphthalene, quinoline, isoquinoline or quinoxaline ring as A.B-ring, were prepared, and their monoamine oxidase (MAO) inhibitory activities were examined. As expected from our previous investigation on the structure-activity relationship of this series, most of them showed strong inhibitory potency to both MAO-A and MAO-B. However, a few indicated highly selective inhibition for either of MAO subtypes.

Animals↗
PubMed1998

[XPS and MS study of phosphorous heterocycle compounds].

7 new phosphorous heterocycle compounds have been studied by XPS and MS. From XPS and MS data we have discussed the existence form and manner of the compounds isomer, and verified that the isomer only exists in gaseous state and liquid state.

English Abstract↗
PubMed2002

Antioxidative activity of heterocyclic compounds found in coffee volatiles produced by Maillard reaction.

Typical heterocyclic compounds substituted with various functional groups found in Maillard reaction products were examined for antioxidant activity. Pyrroles exhibited the greatest antioxidant activity among all heterocyclic compounds tested. All pyrroles inhibited hexanal oxidation by almost 100% at a concentration of 50 microg/mL over 40 days. Addition of formyl and acetyl groups to a pyrrole ring enhanced antioxidative activity remarkably. Pyrrole-2-carboxaldehyde, 2-acetylpyrrole, 1-methyl-2-pyrrolecarboxaldehyde, and 2-acetyl-1-methylpyrrole inhibited hexanal oxidation by >80% at 10 microg/mL. Unsubstituted furan exhibited the greatest antioxidant activity among furans tested. Addition of all functional groups used in this study to furan decreased antioxidative activity. The antioxidant activity of thiophene increased with the addition of methyl and ethyl groups, but the addition of formyl or acetyl groups to thiophene decreased antioxidant activity. Thiazoles and pyrazines were ineffective antioxidants at all concentrations tested. Reaction of all heterocyclic compounds with hydrogen peroxide resulted in the formation of various oxidized products.

Aldehydes↗
PubMed1993

[Anxiolytic activities of pentanthrene type heterocyclic compounds].

A series of pentanthrene type heterocyclic compounds were synthesized and evaluated for anxiolytic activities by three kinds of behavioral pharmacological tests. Several compounds showed anxiolytic activities. In particular, s-triazolo[3,4-a]phthalazine (Tri-P) and 3-propyl derivatives of Tri-P(PTP) showed remarkable activities, although the activities were slightly lower than those of diazepam. The results suggested that Tri-P or PTP is a useful lead compound for the development of the antianxietic agents. The relationship between the structure and anxiolytic activity, and the inducing mechanism of the activity was discussed.

Animals↗
PubMed2000

Antioxidative activities of heterocyclic compounds formed in brewed coffee.

Typical volatile heterocyclic compounds found in brewed coffee extracts-pyrroles, furans, thiophenes, and thiazoles-were examined for antioxidative activity, which was determined by measuring the oxidative conversion of hexanal to hexanoic acid using gas chromatography. 2-Acetylpyrrole, 1-methylpyrrole, and pyrrole inhibited hexanal oxidation by 98, 87, and 78%, respectively, at a concentration of 500 microgram/mL over a period of 30 days. 2-Methylfuran, which inhibited hexanal oxidation by 90% at all concentrations tested (500, 200, and 100 microgram/mL) for a 30-day period, exhibited the greatest activity among furans tested. Similarly, 2-methylthiophene, which inhibited hexanal oxidation by almost 100% at a concentration of 500 microgram/mL over 30 days, exhibited the greatest activity among the thiophenes tested. In general, thiazoles were ineffective antioxidants at all concentrations tested. However, 4,5-dimethylthiazole was able to inhibit hexanal oxidation by 50% at the highest level tested (500 microgram/mL). 2-Acetylpyrrole, 2-methylfuran, and 2-methylthiophene at concentrations of 500, 200, and 100 microgram/mL and furan at a concentration of 500 microgram/mL exhibited antioxidative activities comparable to that of the synthetic antioxidant butylated hydroxytoluene at a concentration of 50 microgram/mL.

Aldehydes↗
PubMed1980

Structure-toxicity relationships of selected nitrogenous heterocyclic compounds.

A series of eleven nitrogen-containing heterocyclic compounds, which may be potentially associated with aqueous effluents from coal conversion technologies, were examined to determine the relationships between their n-octanol/H2O partition coefficients, molecular weights, boiling points, and their toxicity monitored as reproduction impairment to Tetrahymena pyriformis. Toxicity increases linearly with increased partition coefficient, molecular weight, and boiling point. All of these parameters increase with increased alkyl and ring addition.

Animals↗
PubMedDate not supplied

Solid-phase synthesis of bis-heterocyclic compounds from resin-bound orthogonally protected lysine.

An efficient method for the solid-phase synthesis of bis-heterocyclic compounds from resin-bound orthogonally protected lysine is presented. The initial reaction step involves the exhaustive reduction of resin-bound tetra-amides using borane-THF, followed by cyclization of the resulting tetra-amine with either carbonyldiimidazole, thiocarbonyldiimidazole, or oxalyldiimidazole to generate resin-bound bis-cyclic ureas, bis-cyclic thioureas, and bis-cyclic diketopiperazines, respectively. Cleavage from the solid support using hydrogen fluoride, followed by extraction and lyophilization, yields the desired bis-heterocyclic compounds in excellent yield and high purity.

Acylation↗