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isoquinoline/sarkoma
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Evaluation of antitumor efficacy and toxicity of novel 6-nitro-2-(3-chloropropyl)-1H-benz[de]isoquinoline-1,3-dione in vivo in mouse.
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OBJECTIVE
This study was aimed to assess the in vivo anti-tumoral potency of the novel 6-nitro-2-(3-chloropropyl)-1H-benz[de]isoquinoline-1,3-dione [Compound 1] that has earlier demonstrated excellent cytotoxicity in 15 out of 17 human tumor cell lines tested.
METHODS
Two murine tumors namely
Anticancer Efficacy of the Combination of Berberine and PEGylated Liposomal Doxorubicin in Meth A Sarcoma-Bearing Mice.
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Berberine, the main isoquinoline alkaloid obtained from traditional plants, e.g., Berberis, Coptis, Coscinium spps., etc., is known to exhibit anticancer activity in vitro and in vivo. In this study, the anticancer potential of berberine combined with PEGylated liposomal doxorubicin (polyethylene
Antitumor efficacy and apoptotic activity of substituted chloroalkyl 1H-benz[de]isoquinoline-1,3-diones: a new class of potential antineoplastic agents.
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A series of ten chloroalkyl 1H-benz[de]isoquinoline-1,3-diones (naphthalimides) were synthesized and evaluated for antitumor activity. Amongst them, new compounds 2d and 2i carrying a 6-NO(2) substituent in the aromatic portion of the molecule possessed significant antineoplastic activity. The most
Trabectedin in soft tissue sarcomas.
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Trabectedin (Yondelis®; PharmaMar, Madrid, Spain), a synthetic anticancer agent originally isolated from the Caribbean tunicate, Ecteinascidia turbinata, is currently approved in more than 70 countries worldwide for the treatment of soft tissue sarcoma (STS). Trabectedin is an isoquinoline
Inactivation and inhibition of Rous sarcoma virus by copper-binding ligands: thiosemicarbazones, 8-hydroxyquinolines, and isonicotinic acid hydrazide.
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We have shown that three types of copper-binding ligands, thiosemicarbazones, 8-hydroxyquinolines, and isonicotinic acid hydrazide and their copper complexes, inactivate the transforming ability of RSV and inhibit its RNA-dependent DNA polymerases. Three other compounds, 2-pyridine
The isoquinoline sulfonamide H7 attenuates radiation-mediated protein kinase C activation and delays the onset of x-ray-induced G2 arrest.
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Protein kinase C activation by ionizing radiation in human tumor cell lines participates in the transcriptional activation of genes which may be associated with the phenotypic response of cells to x-rays. We gamma-irradiated cell line RIT-3 (radiation-induced human sarcoma) and quantified the
PARP1 expression drives the synergistic antitumor activity of trabectedin and PARP1 inhibitors in sarcoma preclinical models.
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Enhancing the antitumor activity of the DNA-damaging drugs is an attractive strategy to improve current treatment options. Trabectedin is an isoquinoline alkylating agent with a peculiar mechanism of action. It binds to minor groove of DNA inducing single- and double-strand-breaks. These kinds of
Evidence for involvement of the protein kinase C pathway in the activation of p37v-mos protein kinase.
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Protein kinases are known to undergo phosphorylation to regulate their activity. To determine whether the protein kinase activity of p37v-mos was similarly regulated, we investigated the influence of two well known protein kinases, namely protein kinase C and protein kinase A, on the activity of
Evaluation of naphthal-NU, a 2-chloroethylnitrosourea derivative of naphthalimide, as a mixed-function anticancer agent.
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Naphthal-NU, 2-[2-[3-(2-chloroethyl)-3-nitrosoureido]ethyl]-1H-benz[de]isoquinoline-1,3-dione (Compound 1) has been synthesized as a rationally designed new mixed-function anticancer agent from 1,8-naphthalic anhydride. Its chemical alkylating activity compared with CCNU as standard compound
Evaluation of naphthalmustine, a nitrogen mustard derivative of naphthalimide as a rationally-designed anticancer agent.
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Naphthalmustine, 2-[2-[bis-(2-chloroethyl)amino]ethyl]-1H-benz[de]isoquinoline-1,3-dione (Compound 1) has been synthesized as a rationally designed new anticancer agent from N-(2-bromoethyl)naphthalimide. Its chemical alkylating activity exceeded that of nor-HN2 used as standard compound for
Antitumor effect of berberine against primary effusion lymphoma via inhibition of NF-κB pathway.
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Primary effusion lymphoma (PEL) is an infrequent and distinct entity among the aggressive non-Hodgkin B cell lymphomas that occurs predominantly in patients with advanced AIDS. It shows serous lymphomatous effusion in body cavities, and is resistant to conventional chemotherapy with a poor
Antitumor activity of N-heterocyclic carboxaldehyde thiosemicarbazone derivatives.
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Antitumor activity of N-heterocyclic carboxaldehyde thiosemicarbazone derivatives was examined in ascites sarcoma-180 system. Among isoquinoline-1-carboxaldehyde thiosemicarbazone derivatives, the parent compound, IQ-1, was the most active and less toxic. On the other hand, among the
Antineoplastic and biochemical properties of arylsulfonylhydrazones of 2-formylpyridine N-oxide.
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The structural parameters necessary for the antineoplastic potency of a new class of anticancer agents, arylsulfonylhydrazones of 2-formylpyridine N-oxide, were examined in mice bearing Sarcoma 180 ascites cells. The findings indicated that (a) replacement of the pyridine ring with benzene,
Synthesis and DNA binding properties of novel benzo[b]isoquino[2,3-h]-naphthyridines.
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Several benzo[b]isoquino[2,3-h]-naphthyridines have been prepared via formal hetero-Diels Alder reaction of N-aryl imines as a key step. These compounds have different side chains at C-11, and a cis or trans configuration at the C-8a,C-14a ring junction. Binding constants for the interaction with
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