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pyrrolidine/kanker
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Effects of N-nitrosopyrrolidine, nitrite and pyrrolidine on tumour development in mice as related to ingestion of cured meat.
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The incidence of tumours in mice fed a standard chow diet and given either N-nitrosopyrrolidine (NPyr), nitrite (NO(2)) or nitrite plus pyrrolidine (NO(2) + Pyr) in the drinking water for 12 months at 100mg, 1 g and 1 g plus 100mg/litre, respectively, was compared with that for a control group (C)
Anti-tumor effect of 3-amino-N-substituted-pyrrolidine-2,5-dione-N-mustard hydrochloride.
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The anti-tumor effect of 3-amino-N-substituted pyrrolidine-2,5-dione-N-mustard hydrochloride (PNM.HCl) against Ehrlich (ascites) carcinoma (EAC) was studied. A substantial increase in the survival of mice bearing EAC tumor was achieved following daily administration of PNM.HCl at subtoxic dosages.
Functionalized pyrrolidine inhibitors of human type II alpha-mannosidases as anti-cancer agents: optimizing the fit to the active site.
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Refining the chemical structure of functionalized pyrrolidine-based inhibitors of Golgi alpha-mannosidase II (GMII) to optimize binding affinity provided a lead molecule that demonstrated nanomolar competitive inhibition of alpha-mannosidases II and an optimal fit in the active site of Drosophila
Synergistic cytotoxic effect of sulindac and pyrrolidine dithiocarbamate against ovarian cancer cells.
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Sulindac, a non-steroidal anti-inflammatory drug, suppresses carcinogenesis and inhibits growth of tumor cells. Pyrrolidine dithiocarbamate (PDTC), a potent NF-κB inhibitor, has been also identified as a potential anti-neoplastic agent. We hypothesized that combination of sulindac and PDTC could
Facile one-pot synthesis of novel dispirooxindole-pyrrolidine derivatives and their antimicrobial and anticancer activity against A549 human lung adenocarcinoma cancer cell line.
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Novel dispirooxindole-pyrrolidine derivatives have been synthesized through 1,3-dipolar cycloaddition of an azomethine ylide generated from isatin and sarcosine with the dipolarophile 3-(1H-indol-3-yl)-3-oxo-2-(2-oxoindolin-3-ylidene)propanenitrile, and also spiro compound of acenaphthenequinone
Enhanced activity of anticancer drugs in murine tumours by co-administration with 3-amino-pyrrolidine-2,5-dione-N-mustard derivative.
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(R,S)3-(N,N-[bis-(2-chloroethyl)]-amino)-1-(2'-methoxyphenyl)- pyrrolidine-2,5-dione hydrochloride (I) has shown antitumor activity against P388 and L1210 leukaemias and Sarcoma 180 (ascites). The effect of (I), when co-administered with anticancer drugs, was studied in these murine tumours.
Fetal bovine serum requirement for pyrrolidine dithiocarbamate-induced apoptotic cell death of MCF-7 breast tumor cells.
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Pyrrolidine dithiocarbamate (PDTC) can form a complex with metal ions and then act as a proteasome inhibitor, which leads to tumor cell apoptosis, and could therefore be developed as an anticancer agent. In our efforts to find factors that induce PDTC-mediated apoptosis of tumor cells, the effect of
Regioselective synthesis of dispiro[1H-indene-2,3'-pyrrolidine-2',3''-[3H]indole]-1,2''(1''H)-diones of potential anti-tumor properties.
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1,3-Dipolar cycloaddition reaction of 2-(arylmethylene)-2,3-dihydro-1H-inden-1-ones 1a-g with non-stabilized azomethine ylides, generated in situ via decarboxylative condensation of isatins 2a,b and sarcosine (3) afforded dispiro[1H-indene-2,3'-pyrrolidine-2',3''-[3H]indole]-1,2''(1''H)-diones 4a-n
Regioselective synthesis and stereochemical structure of anti-tumor active dispiro[3H-indole-3,2'-pyrrolidine-3',3''-piperidine]-2(1H),4''-diones.
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Reaction of 3,5-bis(arylmethylene)-1-methyl-4-piperidinones 1a-1g with azomethine ylides (generated in situ via decarboxylative condensation of isatins 2a,2b with sarcosine 3) in refluxing ethanol afforded
Design, synthesis, and evaluation of novel galloyl pyrrolidine derivatives as potential anti-tumor agents.
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A series of novel galloyl pyrrolidine derivatives were synthesized as potential anti-tumor agents. Their inhibiting activities on gelatinase (MMP-2 and -9) were tested with succinylated gelatin as the substrate. Structure-activity analyses demonstrate that introduction of longer and more flexible
Design, synthesis, and evaluation of pyrrolidine based CXCR4 antagonists with in vivo anti-tumor metastatic activity
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The chemokine receptor CXCR4 has been proposed as a drug target based on its important functions in HIV infection, inflammation/autoimmune diseases and cancer metastasis. Herein we report the design, synthesis and evaluation of novel CXCR4 antagonists based on a pyrrolidine scaffold. The structural
Induction of cell killing and autophagy by amphiphilic pyrrolidine derivatives on human pancreatic cancer cells.
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We have synthesized a wide array of structurally related amphiphilic compounds, containing a functionalized pyrrolidine polar group coupled to different ether-linked hydrocarbon chains, to generate novel structures with antitumor activity. These newly synthesized amphiphilic pyrrolidine-derived
Clioquinol and pyrrolidine dithiocarbamate complex with copper to form proteasome inhibitors and apoptosis inducers in human breast cancer cells.
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BACKGROUND
A physiological feature of many tumor tissues and cells is the tendency to accumulate high concentrations of copper. While the precise role of copper in tumors is cryptic, copper, but not other trace metals, is required for angiogenesis. We have recently reported that organic
Synthesis and biological evaluation of novel pyrrolidine-2,5-dione inhibitors as potential anti-tumour agents.
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Several novel pyrrolidine-2,5-dione based compounds have been synthesised and evaluated for their biological activity against human placental aromatase (AR), rat testicular 17 alpha-hydroxylase/17,20-lyase (P450(17) alpha) and bovine cholesterol side chain cleavage (CSCC). The compounds showed good
Nonhormonal selective estrogen receptor modulator 1-(2-[4-{(3R,4S)-7-Methoxy-2, 2-dimethyl-3-phenyl-chroman-4yl}phenoxy]ethyl)pyrrolidine hydrochloride (ormeloxifene hydrochloride) for the treatment of breast cancer.
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Breast cancer is the most common type of diagnosed cancers in women, difficult to treat, and has received international attention because of its aggressive nature and inherent drug resistance mechanisms. Development of a better selective estrogen receptor modulator with good therapeutic profile and
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