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Design and synthesis of highly active Alzheimer's beta-secretase (BACE1) inhibitors, KMI-420 and KMI-429, with enhanced chemical stability.
TLDR
KMI-420 and KMI-429, containing a tetrazole ring, showed improved stability and potent enzyme inhibitory activity and was used as a bioisostere of the free carboxylic acid of the oxalyl group. Expand
Design and synthesis of antiangiogenic/heparin-binding arginine dendrimer mimicking the surface of endostatin.
TLDR
Two antiangiogenic arginine-rich dendrimers are designed and synthesized, which mimic the surface structure of endostatin and have stronger in vivo antiangIogenic activity at 10 microg/CAM in the chicken embryo chorioallantoic membrane (CAM) assay. Expand
Identification of peptidomimetic HTLV-I protease inhibitors containing hydroxymethylcarbonyl (HMC) isostere as the transition-state mimic.
TLDR
Newly synthesized substrate-based inhibitors containing hydroxymethylcarbonyl (HMC) isostere showed potent anti-HTLV-I PR activity. Expand
Potentially lethal damage repair by total and quiescent tumor cells following various DNA-damaging treatments.
TLDR
Differences in sensitivity between total and Q cells and repair patterns of the two cell populations were thought to depend on differences between the two Cell populations in the toxicity of the DNA-damaging treatment and distribution pattern of the anticancer agent. Expand
KMI-358 and KMI-370, highly potent and small-sized BACE1 inhibitors containing phenylnorstatine.
TLDR
A novel substrate-based octapeptide BACE1 inhibitor KMI-008 containing hydroxymethylcarbonyl (HMC) isostere as a transition-state mimic was designed and synthesized. Expand
KMI-008, a novel beta-secretase inhibitor containing a hydroxymethylcarbonyl isostere as a transition-state mimic: design and synthesis of substrate-based octapeptides.
TLDR
A novel class of substrate-based beta-secretase (BACE1) inhibitors containing a hydroxymethylcarbonyl (HMC) isostere was designed and synthesized and Phenylnorstatine was an effective transition-state mimic at the P(1) position. Expand
Modification of tirapazamine-induced cytotoxicity in combination with mild hyperthermia and/or nicotinamide: reference to effect on quiescent tumour cells.
TLDR
The combination of TPZ and mild heat treatment may be useful for sensitizing tumour cells in vivo, including Q cells, which were greater than those of total tumour cell populations in both tumour systems. Expand
New antimetastatic hypoxic cell radiosensitizers: design, synthesis, and biological activities of 2-nitroimidazole-acetamide, TX-1877, and its analogues.
TLDR
TX-1877 and its analogues are potential antimetastatic hypoxic cell radiosensitizers, which would improve the efficiency of radiotherapy and quality of life in cancer treatment, and the MO data might be useful for designing a bifunctional hyp toxic cell radiosenseitizer. Expand
Design, synthesis, and biological activity of anti-angiogenic hypoxic cell radiosensitizer haloacetylcarbamoyl-2-nitroimidazoles.
TLDR
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
Combined effects of tirapazamine and mild hyperthermia on anti-angiogenic agent (TNP-470) treated tumors-reference to the effect on intratumor quiescent cells.
TLDR
Combined treatment with TPZ and MHT, whether other cytotoxic treatments such as gamma-ray irradiation or chemotherapy using cisplatin were combined or not, was useful for sensitizing tumor cells in vivo including Q cells even after TNP-470 treatment. Expand
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