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A novel weakly DNA-intercalative bioreductive compound. 4-[3-(2-nitro-1-imidazolyl)-propylamino]-7-chloroquinoline hydrochloride (NLCQ-1). has been synthesized and studied as a hypoxia-selective cytotoxin in vitro. NLCQ-1, which shares a similar structure with the DNA-intercalative antimalarial drug chloroquine, bound more strongly to DNA than the(More)
The novel hypoxia-selective cytotoxin NLCQ-1, which is a weak DNA intercalator, was studied in conjunction with radiation against V79 cultured cells and EMT6 or SCCVII tumors in their syngeneic mice and compared with tirapazamine (TPZ). NLCQ-1 was a very potent and efficient radiosensitizer of hypoxic V79 cells, providing SER values of 2.27-2.56 at 20-80(More)
Our recent studies with 9-[3-(2-nitro-1-imidazolyl)propylamino]-1,2,3,4,-tetrahydroacridine++ + hydrochloride (a 2-nitroimidazole-linked 1,2,3,4-tetrahydroacridine derivative) shows that less effective DNA binding indeed leads to a hypoxic radiosensitizer and cytotoxin of superior in vitro therapeutic index to the fully aromatic nitroimidazole-linked(More)
9-(3-(2-Nitro-1-imidazolyl)propylamino]-cyclopentano[b]quinoline hydrochloride (NLCPQ-1) is one member of a limited series of 2-nitroimidazole-linked derivatized quinolines we have synthesized to be weak DNA binding compounds. On a concentration basis, NLCPQ-1 is the most potent analogue of the series as a radiosensitizer and cytotoxin of hypoxic cells in(More)
The enzymatic cell-free metabolism of the novel hypoxia-selective cytotoxin 4-[3-(2-nitro-1-imidazolyl)-propylamino]-7-chloroquinoline hydrochloride (NLCQ-1) was investigated under hypoxic or aerobic conditions in the presence of purified reductive enzymes or isolated rat liver microsomes by monitoring the parent compound with HPLC-UV analysis. Enzymatic(More)
Ricin is a toxic protein present in the seeds of castor bean plant. It can be inactivated by heat; therefore characterization of denatured ricin is essential to differentiate it from native ricin and to avoid any ambiguity in its identification. In this study, potential of mass spectrometry using MALDI—TOF/MS has been exploited to investigate the(More)
19F-labeled bioreductive drugs bound to hypoxic cells in tumors could be detected by nuclear magnetic resonance, provided that they do not lose 19F during their metabolism. NLTQ-1, a 2-nitroimidazole-linked 7-trifluoromethylquinoline, has been synthesized to furnish this aim. NLTQ-1 demonstrated hypoxic selectivities of 7-10 in various cell-lines, in vitro.(More)
Sarin is a highly toxic organophosphonate and neural enzyme acetylcholinesterase (AChE) inhibitor. Inhibition of AChE causes large accumulation of acetylcholine at synaptic cleft leading to hyper activation of nicotinic and muscarinic acetylcholine receptors, causing excessive secretions, muscle fasciculation, nausea, vomiting, respiratory distress and(More)
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