Gaosheng S. Xie

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The synthesis, characterization, inhibitory activity against topoisomerase I, and biological evaluation of a series of oligopeptide-substituted bisindolylmaleimides 7-12 are described. Compounds 7-9, which contain a basic C-terminus function such as (dimethylamino)propyl and bind to DNA with C(50) values of 200, 160, and 135 microM, respectively, exhibited(More)
The design and synthesis of certain oligopeptides structurally related to distamycin and netropsin, but bearing mixed heterocyclic moieties capable of recognizing alternative base sites and nitrogen mustard moieties capable of covalent binding to DNA, are described. The binding and thermally induced DNA cleavage, covalent interstrand cross-linking, DNA(More)
A series of hybrids, 4-13, incorporating propargylic sulfones and minor groove-binding oligopeptide carriers, was synthesized. The anticipated preferential binding at adenine sites within the minor groove was confirmed by sequencing determination of these agents on high-resolution gels, indicating preferential alkylation at guanine, and significantly, high(More)
OBJECTIVE To compare the trichloroethylene (TCE) -induced alteration in cell proliferation, cell apoptosis, histone deacetylase activity and expression levels in human hepatic L-02 cells (L-02 cells) and SET deficient cells, and reveal the TCE-induced effect in histone modification and the role of SET on epigenetic pathway. METHODS The L-02 cells and(More)
Novel DNA-directed alkylating agents comprising naphthalimide, nitrogen mustard and lexitropsin moieties have been designed, synthesized and characterized. Their properties have been evaluated with respect to DNA binding ability, sequence preference, influence of flanking sequences on alkylation efficiency and cytotoxic potency against KB human(More)
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