154 research outputs found
A Model for NAD(P)H:Quinoneoxidoreductase 1 (NQO1) Targeted Individualized Cancer Chemotherapy
NQO1 (NAD(P)H:quinoneoxidoreductase 1) is a reductive enzyme that is an important activator of bioreductive antitumor agents. NQO1 activity varies in individual tumors but is generally higher in tumor cells than in normal cells. NQO1 has been used as a target for tumor specific drug development. We investigated a series of bioreductive benzoquinone mustard analogs as a model for NQO1 targeted individualized cancer chemotherapy. We compared the tumor cell growth inhibitory activity of benzoquinone mustard analogs with sterically bulky groups of different size and placed at different positions on the benzoquinone ring, using tumor cell lines with different levels of NQO1. We demonstrated that functional groups of different steric size could be used to produce a series of bioreductive antitumor agents that were activated by different levels of NQO1 in tumor cells. This series of drugs could then be used to target cells with specific levels of NQO1 for growth inhibition and to avoid damage to normal cells, like bone marrow cells, that have low levels of NQO1. This approach could be used to develop new bioreductive antitumor agents for NQO1 targeted individualized cancer chemotherapy
1,3-Benzothiazole-2(3H)-selone
The title compound, C7H5NSSe, is the product of the reaction of 2-chlorobenzothiazole with sodium hydroselenide. The molecule is almost planar (r.m.s. deviation = 0.018 Å) owing to the presence of the long chain of conjugated bonds (Se=C—N—C=C—C=C—C=C). The geometrical parameters correspond well to those of the analog N-methylbenzothiazole-2(3H)-selone, demonstrating that the S atom does not take a significant role in the electron delocalization within the molecule. In the crystal, molecules form centrosymmetric dimers by means of intermolecular N—H⋯Se hydrogen bonds. The dimers have a nonplanar ladder-like structure. Furthermore, the dimers are linked into ribbons propagating in [010] by weak attractive Se⋯S [3.7593 (4) Å] interactions
ChemInform Abstract: THERMAL AND PHOTOCHEMICAL STUDIES OF SYMMETRICAL AND UNSYMMETRICAL DIHYDRO-1,3,4-SELENADIAZOLES
ChemInform Abstract: Functions Containing a Selenocarbonyl or Tellurocarbonyl Group-SeC(X)X′ and TeC(X)X′
ChemInform Abstract: TWOFOLD EXTRUSION REACTIONS OF SELONES AND AZIDES: THE PREPARATION OF VERY STERICALLY HINDERED IMINES
ChemInform Abstract: A Directed Metalation Route to the Selenium Analogue of Methimazole.
ChemInform Abstract: Key Intermediates for the Synthesis of Organic Semiconductors: A Direct Dithiocarbamate Route to Unsubstituted 1,3-Dithiol-2-one Derivatives.
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