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Angiogenesis inhibitor TX-1898: syntheses of the enantiomers of sterically diverse haloacetylcarbamoyl-2-nitroimidazole hypoxic cell radiosensitizers.
R-p-tert-butylphenyl-bromoacetylcarbamoyl-2-nitroimidazole, TX-1898, was found to be the most promising candidate for further development of as anti-angiogenic hypoxic cell radiosensitizer. Expand
Design, synthesis, and biological activity of anti-angiogenic hypoxic cell radiosensitizer haloacetylcarbamoyl-2-nitroimidazoles.
The in vivo chick CAM angiogenesis assay showed that the strong bromoacetylcarbamoyl-2-nitroimidazole radiosensitizers, such as TX-1845 andTX-1846, were the strongest angiogenic inhibitors among them. Expand
Design of antiangiogenic hypoxic cell radiosensitizers: 2-nitroimidazoles containing a 2-aminomethylene-4-cyclopentene-1,3-dione moiety.
These chiral 2-nitroimidazole derivatives that contain the 2-aminomethylene-4-cyclopentene-1,3-dione moiety as a potent antiangiogenic pharmacophoric descriptor are promising lead candidates for the development of antiangsiogenic hypoxic cell radiosensitizers. Expand
Synthesis and biological evaluation of hypoxia-activated prodrugs of SN-38.
Improved the method of multi-gram scale synthesis of (1-methyl-2-nitro-1H-imidazol-5-yl)methanol, which increased the yield to 42% compared to 8% by the original synthesis method, was used to synthesize evofosfamide (TH-302) and hypoxia-activated prodrugs of SN-38. Expand
Synthesis and Biological Evaluation of Paclitaxel and Camptothecin Prodrugs on the Basis of 2-Nitroimidazole.
In this letter, PTX and SN-38 were attached to the N-1 position of 2-nitroimidazole via a carbonate linker and exhibited a considerable stability in buffers at different pH values as well as in human plasma. Expand
Selective turn-on near-infrared fluorescence probe for hypoxic tumor cell imaging
Hypoxia is a typical feature of solid tumors. To detect hypoxic tumor cells, we designed new selective turn-on probes by conjugating (1-methyl-2-nitro-1H-imidazol-5-yl)methanol to the near-infraredExpand
Synthesis of New Branched 2-Nitroimidazole as a Hypoxia Sensitive Linker for Ligand-Targeted Drugs of Paclitaxel
A new bioreductive linker based on 2-nitroimidazole, which was used in three paclitaxel (PTX) prodrugs, was designed and synthesized and was promising in the development of ligand-targeted drugs. Expand
Protective effect of carnosic acid and its semisynthetic derivatives against H2O2-induced neurotoxicity
Abstract Carnosic acid and its new derivatives (17 in total) were tested for their protective effects on hippocampal neuron against H2O2-induced damage using cell counting kit-8. Carnosic acid andExpand
2D/3D-QSAR Studies of [1,2,4]Triazolo[1,5-a]pridinylpyridine Derivatives as Potent Anticancer Agents
By using a combined method of density functional theory(DFT), molecular mechanics(MM2) and statistics for two-dimensional(2D), as well as the comparative molecular field analysis(Co MFA) andExpand