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Pteridine-binding alpha 1-acid glycoprotein from blood of patients with neoplastic diseases.

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A glycoprotein was selectively enriched in the supernatant (Fraction b) obtained by alcohol and trichloroacetic acid fractionation of digitonin extracts from blood of patients with neoplastic diseases and of control subjects. Subsequent chromatography with concanavalin A:Sepharose separated a

[Pteridine metabolism in the ascites tumor cell and the host animal of Yoshida sarcoma (author's transl)].

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Determination of pteridines in biological samples with an emphasis on their stability.

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Pteridines are a group of endogenous heterocyclic compounds whose concentrations in biological fluids may be increased in some disorders, such as infections, autoimmune disorders and cancer. In particular, pteridine concentrations in urine may represent promising noninvasive markers. However, their

Synthesis and in vitro evaluation of 2-amino-4-N-piperazinyl-6-(3,4-dimethoxyphenyl)-pteridines as dual immunosuppressive and anti-inflammatory agents.

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Screening of a pteridine-based compound library led to the identification of compounds exhibiting immunosuppressive as well as anti-inflammatory activity. Optimization afforded a series of 2-amino-4-N-piperazinyl-6-(3,4-dimethoxyphenyl)pteridine analogues. The most potent congeners in this series

Pteridine-2,4-diamine derivatives as radical scavengers and inhibitors of lipoxygenase that can possess anti-inflammatory properties.

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BACKGROUND Reactive oxygen species are associated with inflammation implicated in cancer, atherosclerosis and autoimmune diseases. The complex nature of inflammation and of oxidative stress suggests that dual-target agents may be effective in combating diseases involving reactive oxygen

Controlled synthesis of mixed molecular nanostructures from folate and deferrioxamine-Ga(III) on gold and tuning their performance for cancer cells.

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A new strategy is developed for construction of the mixed molecular nanostructures from folic acid (FOA), a targeting agent, and deferrioxamoine-Ga(III), (DFO-Ga(III)), a theranostic agent, on gold-mercaptopropionic acid surface, Au-MPA. The strategy is focused to achieve a system in which all the

Anti-leukemia activity of 4-amino-2-aryl-6,9-dichlorobenzo[g]pteridines.

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Pteridines are bicyclic heterocyclic compounds with a pyrazino[2,3-d]pyrimidine nucleus that have shown a wide range of therapeutic utilities. Concretely, 4-aminopteridine derivatives have demonstrated both anti-inflammatory and anti-cancer properties, and some of them, such as methotrexate, are

2,4-Diamino-6-(bis-2-chloroethyl)aminomethyl pteridine. A new potent anticancer drug.

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2,4-Diamino-6-(bis-2-chloroethyl)aminomethyl pteridine has been synthesized and found to be highly potent against L-1210 mouse leukemia lymphoblasts. A single dose of 5 mg/kg injected 24 h after the tumor inoculation increased the life-span of 50% of mice to more than 200%, while the other 50% of

Synthesis and structure-activity relationships of pteridine dione and trione monocarboxylate transporter 1 inhibitors.

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Novel substituted pteridine-derived inhibitors of monocarboxylate transporter 1 (MCT1), an emerging target for cancer therapy, are reported. The activity of these compounds as inhibitors of lactate transport was confirmed using a (14)C-lactate transport assay, and their potency against

Exploring the inhibitory activity of Withaferin-A against Pteridine reductase-1 of L. donovani.

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Withaferin A is an abundant withanolide present in Withania somnifera leaves and to some extent in roots. It has been known for its profound anti-cancer properties, but its role in counteracting the Leishmania donovani infection has to be explored. Pteridine reductase 1 (PTR1) is involved in

Pteridine-sulfonamide conjugates as dual inhibitors of carbonic anhydrases and dihydrofolate reductase with potential antitumor activity.

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Recent evidences suggest that cancer treatment based on combination of cytostatic and conventional chemostatic therapeutics, which are usually cytotoxic, can provide an improved curative option. On the sequence of our previous work on methotrexate (MTX) derivatives, we have developed and evaluated

Substituted xanthines, pteridinediones, and related compounds as potential antiinflammatory agents. Synthesis and biological evaluation of inhibitors of tumor necrosis factor alpha.

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A series of analogues of pentoxifylline metabolites were prepared in the purine, pteridine, [1,2,5]-thiadiazolo[3,4-d]pyrimidine, and quinazoline ring systems and evaluated for their ability to inhibit the production of tumor necrosis factor-alpha (TNF alpha) in human peripheral blood monocytes

Design, synthesis, and biological evaluation of 4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridine derivatives as novel dual-PLK1/BRD4 inhibitors.

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Protein kinase inhibitors and epigenetic regulatory molecules are two main kinds of anticancer drugs developed in recent years. Both kinds of drugs harbor their own advantages and disadvantages in the treatment of cancer, and the development of small molecules which could target at kinases and

Anti-inflammatory activity of a pteridine derivative (4AZA2096) alleviates TNBS-induced colitis in mice.

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Elevated production of tumor necrosis factor (TNF) plays a central role in the pathogenesis of many inflammatory diseases, such as rheumatoid arthritis and Crohn's disease. Naturally occurring pteridine analogs have been reported to have potent immunomodulatory activity, especially on TNF

CoMFA and CoMSIA 3D-QSAR analysis of DMDP derivatives as anti-cancer agents.

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Comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) based on three dimensional quantitative structure-activity relationship (3D-QSAR) studies were conducted on a series (78 compounds) of 2, 4-diamino-5-methyl-5-deazapteridine (DMDP) derivatives

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