- Kawase

Summary

Affiliation: Josai University
Country: Japan

Publications

  1. ncbi request reprint Convenient synthesis of alpha-trifluoromethylated acyloins from alpha-hydroxy or alpha-amino acids
    M Kawase
    Faculty of Pharmaceutical Sciences, Josai University, Sakado, Saitama, Japan
    Chem Pharm Bull (Tokyo) 48:1338-43. 2000
  2. ncbi request reprint Coumarin derivatives with tumor-specific cytotoxicity and multidrug resistance reversal activity
    Masami Kawase
    Faculty of Pharmaceutical Sciences, Josai University, Saitama, Japan
    In Vivo 19:705-11. 2005
  3. ncbi request reprint Structural requirements of hydroxylated coumarins for in vitro anti-Helicobacter pylori activity
    Masami Kawase
    Faculty of Pharmaceutical Sciences, Josai University, 1 1 Keyakidai, Sakado, Saitama 350 0295, Japan
    In Vivo 17:509-12. 2003
  4. ncbi request reprint Structure-cytotoxic activity relationships of simple hydroxylated coumarins
    Masami Kawase
    Faculty of Pharmaceutical Sciences, Josai University, Sakado, Saitama 350 0295, Japan
    Anticancer Res 23:3243-6. 2003
  5. ncbi request reprint Biological activity of persimmon (Diospyros kaki) peel extracts
    Masami Kawase
    Faculty of Pharmaceutical Sciences, Josai University, Sakado, Saitama, Japan
    Phytother Res 17:495-500. 2003
  6. ncbi request reprint New multidrug resistance reversal agents
    Masami Kawase
    Faculty of Pharmaceutical Sciences, Josai University, Saitama, Japan
    Curr Drug Targets 4:31-43. 2003
  7. ncbi request reprint Cell death-inducing activity of opiates in human oral tumor cell lines
    Masami Kawase
    Faculty of Pharmaceutical Sciences, Josai University, Sakado, Saitama, Japan
    Anticancer Res 22:211-4. 2002
  8. ncbi request reprint 3,5-dibenzoyl-1,4-dihydropyridines: synthesis and MDR reversal in tumor cells
    Masami Kawase
    Faculty of Pharmaceutical Sciences, Josai University, 350 0295, Saitama, Japan
    Bioorg Med Chem 10:1051-5. 2002
  9. ncbi request reprint Convenient synthesis of 4-trifluoromethyl-substituted imidazole derivatives
    M Kawase
    Faculty of Pharmaceutical Sciences Josai University, Sakado, Saitama, Japan
    Chem Pharm Bull (Tokyo) 49:461-4. 2001
  10. ncbi request reprint Antimicrobial activity of trifluoromethyl ketones and their synergism with promethazine
    M Kawase
    Faculty of Pharmaceutical Sciences, Josai University, Sakado, Saitama 350 0295, Japan
    Int J Antimicrob Agents 18:161-5. 2001

Collaborators

Detail Information

Publications64

  1. ncbi request reprint Convenient synthesis of alpha-trifluoromethylated acyloins from alpha-hydroxy or alpha-amino acids
    M Kawase
    Faculty of Pharmaceutical Sciences, Josai University, Sakado, Saitama, Japan
    Chem Pharm Bull (Tokyo) 48:1338-43. 2000
    ..The reaction of 1 with TFAA shows more potential for practical applications because of the ready availability of the starting materials and ease of manipulation...
  2. ncbi request reprint Coumarin derivatives with tumor-specific cytotoxicity and multidrug resistance reversal activity
    Masami Kawase
    Faculty of Pharmaceutical Sciences, Josai University, Saitama, Japan
    In Vivo 19:705-11. 2005
    ..A deeper understanding of the relationship between their structures and their potency will contribute to the design of optimal agents...
  3. ncbi request reprint Structural requirements of hydroxylated coumarins for in vitro anti-Helicobacter pylori activity
    Masami Kawase
    Faculty of Pharmaceutical Sciences, Josai University, 1 1 Keyakidai, Sakado, Saitama 350 0295, Japan
    In Vivo 17:509-12. 2003
    ..In hydroxylated coumarins, the methyl group at C-4 position enhanced the activity. The inhibitory activity of coumarins (1-23) against jack bean urease was examined, but no coumarins showed any inhibition at 160 micrograms/mL...
  4. ncbi request reprint Structure-cytotoxic activity relationships of simple hydroxylated coumarins
    Masami Kawase
    Faculty of Pharmaceutical Sciences, Josai University, Sakado, Saitama 350 0295, Japan
    Anticancer Res 23:3243-6. 2003
    ..Agarose gel electrophoresis revealed that esculetin and its derivatives with tumor-specific cytotoxicity induce internucleosomal DNA fragmentation in HL-60 cells...
  5. ncbi request reprint Biological activity of persimmon (Diospyros kaki) peel extracts
    Masami Kawase
    Faculty of Pharmaceutical Sciences, Josai University, Sakado, Saitama, Japan
    Phytother Res 17:495-500. 2003
    ..These results indicate the therapeutic value of persimmon peel extracts as potential antitumor and MDR-reversing agents...
  6. ncbi request reprint New multidrug resistance reversal agents
    Masami Kawase
    Faculty of Pharmaceutical Sciences, Josai University, Saitama, Japan
    Curr Drug Targets 4:31-43. 2003
    ..The use of MDR modulators is a promising approach to overcome the undesired MDR phenotype. The more effective MDR modulators are urgently needed for clinical use. This review focuses on literatures published in 1998-2001...
  7. ncbi request reprint Cell death-inducing activity of opiates in human oral tumor cell lines
    Masami Kawase
    Faculty of Pharmaceutical Sciences, Josai University, Sakado, Saitama, Japan
    Anticancer Res 22:211-4. 2002
    ..These data suggest that codeinone induces cytotoxicity in oral tumor cell lines, possibly by a Michael-like addition of a protein SH or of an amino group to the bouble bond of codeinone...
  8. ncbi request reprint 3,5-dibenzoyl-1,4-dihydropyridines: synthesis and MDR reversal in tumor cells
    Masami Kawase
    Faculty of Pharmaceutical Sciences, Josai University, 350 0295, Saitama, Japan
    Bioorg Med Chem 10:1051-5. 2002
    ..These data suggest that 3,5-dibenzoyl-4-(3-chlorophenyl)-1,4-dihydro-2,6-dimethylpyridine (12) can be recommended as a new drug candidate for MDR cancer treatment...
  9. ncbi request reprint Convenient synthesis of 4-trifluoromethyl-substituted imidazole derivatives
    M Kawase
    Faculty of Pharmaceutical Sciences Josai University, Sakado, Saitama, Japan
    Chem Pharm Bull (Tokyo) 49:461-4. 2001
    ..Dehydration of 3 gives 4-trifluoromethylimidazoles (4) in high yields. The novel ring transformation of 1 into 3 occurs via a regioselective attack of ammonia on the C-2 position of the ring...
  10. ncbi request reprint Antimicrobial activity of trifluoromethyl ketones and their synergism with promethazine
    M Kawase
    Faculty of Pharmaceutical Sciences, Josai University, Sakado, Saitama 350 0295, Japan
    Int J Antimicrob Agents 18:161-5. 2001
    ..The inhibition was more marked in the proton pump deficient E. coli mutant than in the wild type, which suggested that the antibacterial effect of trifluoromethyl ketones is partly prevented by the proton pump system...
  11. ncbi request reprint Antimicrobial activity of new coumarin derivatives
    M Kawase
    Faculty of Pharmaceutical Sciences, Josai University, Saitama, Japan
    Arzneimittelforschung 51:67-71. 2001
    ..The presence of phenolic hydroxyl group and/or carboxylic acid was necessary to possess higher activity against Helicobacter pylori...
  12. ncbi request reprint Trifluoromethyl ketone-based inhibitors of apoptosis in cerebellar granule neurons
    - Kawase
    Faculty of Pharmaceutical Sciences, Josai University, Sakado, Saitama, Japan
    Biol Pharm Bull 24:1335-7. 2001
    ..Furthermore, these compounds effectively suppressed DNA fragmentation accompanied with apoptosis. The neuroprotection mode of 2 and 11 was not related to inhibition of caspase-3...
  13. ncbi request reprint Brominations of steroidal hormone having alpha,beta-unsaturated ketone, 17-O-acetyltestosterone, in the presence of silver triflate
    T Shimizu
    Faculty of Pharmaceutical Sciences, Josai University, Sakado, Saitama, Japan
    Chem Pharm Bull (Tokyo) 49:23-8. 2001
    ..The formations of the products were inferred on the basis of products obtained under controlled brominations of 1 in the presence of AgOTf, and of those obtained by the brominations of compounds 9-13 also in the presence of AgOTf...
  14. ncbi request reprint Effect of anticancer agents on codeinone-induced apoptosis in human cancer cell lines
    Risa Takeuchi
    Division of Anesthesiology, Department of Comprehensive Medical Sciences, Meikai University School of Dentistry, Sakado, Saitama 350 0283, Japan
    Anticancer Res 25:4037-41. 2005
    ..These data suggest that codeinone has possible antitumor potential, in addition to its action as a narcotic analgesic, even though it induces incomplete apoptosis-associated characteristics...
  15. ncbi request reprint Induction of non-apoptotic cell death by morphinone in human promyelocytic leukemia HL-60 cells
    Risa Takeuchi
    Division of Anesthesiology, Department of Comprehensive Medical Sciences, Meikai University School of Dentistry, Sakado, Saitama 350 0283, Japan
    Anticancer Res 26:3343-8. 2006
    ..The autophagy inhibitor 3-methyladenine (0.3-10 mM) slightly inhibited the morphinone-induced cytotoxicity, when corrected for its own cytotoxicity. These data suggest that morphinone induces non-apoptotic cell death in HL-60 cells...
  16. ncbi request reprint Multidrug resistance reversal by 3-formylchromones in human colon cancer and human mdr1 gene-transfected mouse lymphoma cells
    Zoltán Baráth
    Institute of Medical Microbiology and Immunobiology, Faculty of General Medicine, University of Szeged, Szeged, Hungary
    In Vivo 20:645-9. 2006
    ..The log P values can provide an adequate explanation for the selective cytotoxicity against cancer cells...
  17. ncbi request reprint Bioactivities of anastasia black (Russian sweet pepper)
    Yoshiaki Shirataki
    Faculty of Pharmaceutical Sciences, Josai University, Sakado, Saitama, Japan
    Anticancer Res 25:1991-9. 2005
    ..These data suggest that Anastasia Black should be further investigated as a potent supplement for cancer chemotherapy...
  18. ncbi request reprint Tumour-specific cytotoxicity and MDR-reversal activity of dihydropyridines
    Helga Engi
    Department of Medical Microbiology and Immunobiology, Albert Szent Gyorgyi Medical Centre, University of Szeged, H 6720 Szeged, Hungary
    In Vivo 20:637-43. 2006
    ..There was no clear-cut relationship between the multidrug-resistance activity or cytotoxicity and the chemical structures of the compounds. New ring substituents could prevent the oxidation of the ring of the aromatic compound...
  19. ncbi request reprint Cytotoxic potential of phenothiazines
    Noboru Motohashi
    Meiji Pharmaceutical University, 2 522 1 Noshio, Kiyose shi, Tokyo 204 8588, Japan
    Curr Drug Targets 7:1055-66. 2006
    ....
  20. ncbi request reprint Tumor-specific cytotoxicity of 3,5-dibenzoyl-1,4-dihydropyridines
    Sufi Reza M D Morshed
    Meikai Pharmaco Medical Laboratory MPL, Meikai University School of Dentistry, Sakado, Saitama, Japan
    Anticancer Res 25:2033-8. 2005
    ..The present study suggests that GB5 and GB12 may induce non-apoptotic cell death in tumor cell lines...
  21. ncbi request reprint Benzo[a]phenoxazines: a new group of potent P-glycoprotein inhibitors
    Olga Wesolowska
    Department of Biophysics, Wroclaw Medical University, ul Chalubinskiego 10, 50 368 Wroclaw, Poland
    In Vivo 20:109-13. 2006
    ..e. to be new effective MDR modulators. The results allowed us to draw preliminary conclusions about the structural features of benzo[a]phenoxazines which are important for MDR modulation...
  22. ncbi request reprint Synergistic interaction between proton pump inhibitors and resistance modifiers: promoting effects of antibiotics and plasmid curing
    Kristina Wolfart
    Department of Medical Microbiology, University of Szeged, 6720 Szeged, Dom ter 10, Hungary
    In Vivo 20:367-72. 2006
    ..coli and that it was this pump which, when inhibited by TF14, allowed more PMZ to reach its plasmid elimination target...
  23. ncbi request reprint Cytotoxic activity of selected trifluoromethyl ketones against oral tumor cells
    Atsushi Ideo
    Division of Oral and Maxillofacial Surgery, Meikai University School of Dentistry, Sakado, Saitama 350 0283, Japan
    Anticancer Res 26:4335-41. 2006
    ..The autophagy inhibitor, 3-methyladenine (3-MA), partially inhibited the TF2- or 3-induced cytotoxicity. These data suggest the induction of non-apoptotic cell death by TF2 or 3...
  24. ncbi request reprint 3-(3,4,5-Trimethoxyphenyl)-1-oxo-2-propene: a novel pharmacophore displaying potent multidrug resistance reversal and selective cytotoxicity
    Umashankar Das
    College of Pharmacy and Nutrition, University of Saskatchewan, 110 Science Place, Saskatoon, Canada SK S7N 5C9
    Bioorg Med Chem 15:3373-80. 2007
    ..In general, they were selectively toxic to malignant rather than normal cells. Two representative compounds induced apoptosis in human HL-60 cells and markedly activated caspase-3...
  25. ncbi request reprint Quantitative structure-cytotoxicity relationship analysis of 5-trifluoromethyloxazole derivatives by a semiempirical molecular-orbital method with the concept of absolute hardness
    Mariko Ishihara
    Division of Basic Chemistry, Meikai University School of Dentistry, Sakado, Saitama 350 0283, Japan
    Anticancer Res 28:997-1003. 2008
    ..The cytotoxic activity of 5-trifluoromethyloxazole derivatives became maximum at log p = 4.6. The concept of absolute hardness is applicable in estimating the cytotoxicity of 5-trifluoromethyloxazoles, using an eta-chi activity diagram...
  26. pmc 1-Aryl-2-dimethylaminomethyl-2-propen-1-one hydrochlorides and related adducts: A quest for selective cytotoxicity for malignant cells
    Hari N Pati
    College of Pharmacy and Nutrition, University of Saskatchewan, 110 Science Place, Saskatoon, Saskatchewan, Canada S7N 5C9
    Bioorg Med Chem 16:5747-53. 2008
    ..The mode of action of a representative compound 1e in HL-60 cells included inducing apoptosis and activation of caspases -3, -8, and -9...
  27. ncbi request reprint Tumor-specificity and type of cell death induced by phenoxazines
    Fumika Suzuki
    Division of Pharmacology, Meikai University School of Dentistry, Sakado, Saitama 350 0283, Japan
    Anticancer Res 27:4233-8. 2007
    ....
  28. ncbi request reprint Tumor-specific cytotoxic activity and type of cell death induced by 4-trifluoromethylimidazoles in human oral squamous cell carcinoma cell lines
    Fumihiro Takekawa
    Division of Pharmacology, Meikai University School of Dentistry, Sakado, Saitama 350 0283, Japan
    Anticancer Res 27:4065-9. 2007
    ..These data suggest that the type of cell death is determined by the type of target cells, but not by the drug-sensitivity of the cells...
  29. ncbi request reprint Quantitative structure-cytotoxicity relationship analysis of phenoxazine derivatives by semiempirical molecular-orbital method
    Mariko Ishihara
    Division of Basic Chemistry, Department of Oral Biology and Tissue Engineering, Meikai University School of Dentistry, Sakado, Saitama 350 0283, Japan
    Anticancer Res 27:4053-7. 2007
    ..27). These data suggest that appropriate chemical descriptors should be selected to estimate the cytotoxicity of phenoxazines, depending on the target cells...
  30. ncbi request reprint Quantitative structure-activity relationship analysis of 4-trifluoromethylimidazole derivatives with the concept of absolute hardness
    Mariko Ishihara
    Division of Basic Chemistry, Department of Oral Biology and Tissue Engineering, Meikai University School of Dentistry, Sakado, Saitama 350 0283, Japan
    Anticancer Res 27:4047-51. 2007
    ..The present study demonstrates that the biological activity of 4-trifluoromethylimidazole derivatives can be estimated by an eta-chi activity diagram...
  31. ncbi request reprint Biological activity of 3-formylchromones and related compounds
    Masami Kawase
    Faculty of Pharmaceutical Sciences, Matsuyama University, 4 2 Bunkyo cho, Matsuyama, Ehime 790 8578, Japan
    In Vivo 21:829-34. 2007
    ..On the other hand, 6,8-dibromo-3-formylchromone (FC11) exhibited potent inhibitory activity against the urease, but had no anti-H. pylori activity. No chromones (FC1-16) exhibited anti-HIV activity...
  32. ncbi request reprint Factors that affect the type of cell death induced by chemicals
    Hiroshi Sakagami
    Department of Diagnostic and Therapeutic Sciences, Meikai University School of Dentistry, Saitama, Japan
    Autophagy 3:493-5. 2007
    ..This suggests that the nature of the chemical structure as well as the type of target cells is another factor that determines the type of cell death induced by chemicals...
  33. pmc Cytotoxic 3,5-bis(benzylidene)piperidin-4-ones and N-acyl analogs displaying selective toxicity for malignant cells
    Hari N Pati
    College of Pharmacy and Nutrition, University of Saskatchewan, 110 Science Place, Saskatoon Saskatchewan S7N 5C9, Canada
    Eur J Med Chem 43:1-7. 2008
    ....
  34. ncbi request reprint Selective toxicity and type of cell death induced by various natural and synthetic compounds in oral squamous cell carcinoma
    Hiroshi Sakagami
    Division of Pharmacology, Department of Oral Diagnostic and Therapeutic Sciences, Meikai University School of Dentistry, Sakado, Saitama 350 0283, Japan
    In Vivo 21:311-20. 2007
    ..Systematization of the relationship between these factors and tumor-specificity may contribute in the quest for more active compounds...
  35. ncbi request reprint Induction of tumor-specific cytotoxicity and apoptosis by doxorubicin
    Fumika Suzuki
    Department of Dental Pharmacology, Meikai University School of Dentistry, Sakado, Saitama 350 0283, Japan
    Anticancer Res 25:887-93. 2005
    ....
  36. ncbi request reprint 3-Arylidene-1-(4-nitrophenylmethylene)-3,4-dihydro-1H-naphthalen-2-ones and related compounds displaying selective toxicity and reversal of multidrug resistance in neoplastic cells
    Jonathan R Dimmock
    College of Pharmacy and Nutrition, University of Saskatchewan, 110 Science Place, Saskatoon, SK, Canada S7N 5C9
    Bioorg Med Chem Lett 15:1633-6. 2005
    ....
  37. ncbi request reprint Relationship between electronic structure and cytotoxic activity of dopamine and 3-benzazepine derivatives
    Teruo Kurihara
    Department of Chemistry, Faculty of Science, Josai University, Sakado, Saitama Japan
    In Vivo 18:443-7. 2004
    ..056 to 2.5 mM) showed the strongest cytotoxic activity with small delta(deltaHf) values, whereas thirteen derivatives [4-8, 10-11, 14-19] (CC50: > 3.6 mM) showed the weakest cytotoxic activity with large delta(deltaHf) values...
  38. pmc 3,5-Dibenzoyl-4-(3-phenoxyphenyl)-1,4-dihydro-2,6-dimethylpyridine (DP7) as a new multidrug resistance reverting agent devoid of effects on vascular smooth muscle contractility
    Simona Saponara
    Istituto di Scienze Farmacologiche, Universita degli Studi di Siena, Via A Moro 2, 53100 Siena, Italy
    Br J Pharmacol 141:415-22. 2004
    ..In conclusion, DP7 may represent a lead compound for the development of potent dihydropyridine MDR chemosensitizers devoid of vascular effects. British Journal of Pharmacology (2004) 141, 415-422. doi:10.1038/sj.bjp.0705635..
  39. ncbi request reprint Inhibition of LPS-stimulated NO production in mouse macrophage-like cells by Barbados cherry, a fruit of Malpighia emarginata DC
    Hidetsugu Wakabayashi
    Faculty of Science, Josai University, Sakado, Saitama 350 0295, Japan
    Anticancer Res 23:3237-41. 2003
    ..These data suggest that the inhibitory effect on NO production by Barbados cherry extracts is partly due to the inhibition of iNOS expression, and scavenging of O2- and NO radicals...
  40. ncbi request reprint Analysis of apoptosis signaling pathway in human cancer cells by codeinone, a synthetic derivative of codeine
    Naoko Hitosugi
    Department of Anesthesiology, Saitama Medical School, Department of Dental Pharmacology, Meikai University School of Dentistry, Saitama, Japan
    Anticancer Res 23:2569-76. 2003
    ..This apoptosis-inducing activity, in conjunction with antinociceptive activity, further substantiated the antitumor potential of codeinone...
  41. ncbi request reprint Cytotoxic and multidrug resistance reversal activity of a vegetable, 'Anastasia Red', a variety of sweet pepper
    Noboru Motohashi
    Meiji Pharmaceutical University, Kiyose, Tokyo, Japan
    Phytother Res 17:348-52. 2003
    ..Thus, this study suggests the effective and selective antitumor potential of 'Anastasia Red' of sweet pepper for further phytochemical and biological investigation...
  42. ncbi request reprint Comparative analysis of apoptosis-inducing activity of codeine and codeinone
    Naoko Hitosugi
    Department of Anesthesiology, Saitama Medical School, Japan
    Anesthesiology 98:643-50. 2003
    ..This was counteracted by an antioxidant, N-acetyl-L-cysteine (NAC). These findings prompted us to perform a more detailed study of apoptosis induction after codeinone treatment...
  43. ncbi request reprint Interaction between various resistance modifiers and apoptosis inducer 12H-benzo[alpha]phenothiazine
    Ilona Mucsi
    Department of Medical Microbiology, Faculty of General Medicine, University of Szeged, Hungary
    Anticancer Res 22:2833-6. 2002
    ..The resistance modifier compounds alone also induced apoptosis and it was slightly higher in the parent cells than its MDR1/A gene-transformed subline...
  44. ncbi request reprint Partial purification of cytotoxic substances from moxa extract
    Ikusuke Hatsukari
    Department of Anesthesiology, Saitama Medical School, Department of Dental Pharmacology, Meikai University School of Dentistry, Saitama, Japan
    Anticancer Res 22:2777-82. 2002
    ..These data suggest that the active principles in the Moxa extract might be different from that in Moxa smoke, which produced carbon radical and modified MnSOD mobility and activity...
  45. ncbi request reprint Interaction between 3,5-diacetyl-1,4-dihydropyridines and ampicillin, and erythromycin on different E. coli strains
    Györgyi Gunics
    Department of Microbiology, Albert Szent Gyorgyi Medical University, Szeged, Hungary
    Int J Antimicrob Agents 20:227-9. 2002
    ..None of the drugs had any effect on a multidrug resistant (MDR) clinical isolate of E. coli Gy-2/Ap(res)Er(res)...
  46. ncbi request reprint Cancer prevention and therapy with kiwifruit in Chinese folklore medicine: a study of kiwifruit extracts
    Noboru Motohashi
    Meiji Pharmaceutical University, 2 522 1 Noshio, Kiyose shi, Tokyo 204 8588, Japan
    J Ethnopharmacol 81:357-64. 2002
    ..All fractions were inactive against Helicobacter pylori. These results demonstrate that gold kiwifruit extracts contain valuable, various bioactive materials, which can be separated with each other...
  47. ncbi request reprint Biological activity of barbados cherry (acerola fruits, fruit of Malpighia emarginata DC) extracts and fractions
    Noboru Motohashi
    Meiji Pharmaceutical University, Noshio, Kiyose, Tokyo, Japan
    Phytother Res 18:212-23. 2004
    ..The tumor specific cytotoxic activity and MDR reversal activity of barbados cherry may suggest its possible application for cancer therapy...
  48. ncbi request reprint Trifluoromethyl ketones show culture age-dependent inhibitory effects on low K(+)-induced apoptosis in cerebellar granule neurons
    Katsuyoshi Sunaga
    Faculty of Pharmaceutical Sciences, Josai University, Sakado, Saitama 350 0295, Japan
    In Vivo 16:97-101. 2002
    ..This study showed that there are different pathways of apoptosis in CGNs depending on the culture age...
  49. ncbi request reprint Biological activity of carotenoids in red paprika, Valencia orange and Golden delicious apple
    Peter Molnar
    Department of Biochemistry and Medical Chemistry, University of Pecs Medical School, Pecs, H 7601 Hungary
    Phytother Res 19:700-7. 2005
    ..The data suggest the potential importance of carotenoids as possible anti-H. pylori and MDR reversal agents. The active principles in the carotenoid extract might differ, depending upon the types of fruits and vegetables...
  50. ncbi request reprint Cytotoxic activity of deferiprone, maltol and related hydroxyketones against human tumor cell lines
    Eiji Yasumoto
    Department of Dental Pharmacology, Meikai University School of Dentistry, Sakado, Saitama, Japan
    Anticancer Res 24:755-62. 2004
    ..HK1 and 3 also activated the caspase 3, 8 and 9 in HSC-2 cells, but to a lesser extent. The present study suggested that the antitumor activity of hydroxyketones may be modified by Fe3+ concentration...
  51. ncbi request reprint Structure-activity relationships of alpha, beta-unsaturated ketones as assessed by their cytotoxicity against oral tumor cells
    Tohru Nakayachi
    Department of Dental Pharmacology, Meikai University School of Dentistry, Sakado, Saitama, Japan
    Anticancer Res 24:737-42. 2004
    ..The study suggests that the presence of a non sterically hindered Michael acceptor seems to be an essential structural requirement for the cytotoxic activity in alpha, beta-unsaturated ketones...
  52. ncbi request reprint Induction of apoptosis by beta-diketones in human tumor cells
    Kensuke Nakano
    Department of Dental Pharmacology, Meikai University School of Dentistry, Sakado, Saitama, Japan
    Anticancer Res 24:711-7. 2004
    ..The tumor-specific cytotoxicity and apoptosis-inducing activity of BD17 against human tumor cells undoubtedly warrant further studies of its efficacy as a cancer chemotherapeutic agent...
  53. ncbi request reprint 3,5-dibenzoyl-4-(3-phenoxyphenyl)-1,4-dihydro-2,6-dimethylpyridine (DP7): a new multidrug resistance inhibitor devoid of effects on Langendorff-perfused rat heart
    Simona Saponara
    Dipartimento di Scienze Biomediche, Universita degli Studi di Siena, Via A Moro 2, 53100 Siena, Italy
    Eur J Pharmacol 563:160-3. 2007
    ..DP7, up to 30 microM, failed to alter ECG parameters. In conclusion, DP7, may represent a lead compound for the development of potent dihydropyridine MDR chemosensitizers devoid of cardiac effects...
  54. ncbi request reprint Effects of trifluoromethyl ketones on the motility of Proteus vulgaris
    Krisztina Wolfart
    Department of Medical Microbiology, Faculty of General Medicine, University of Szeged, Szeged, H 6720, Hungary
    Biol Pharm Bull 27:1462-4. 2004
    ....
  55. ncbi request reprint Determination of lipid bilayer/water partition coefficient of new phenothiazines using the second derivative of absorption spectra method
    Andrzej Poła
    Department of Biophysics, Wrocław Medical University, ul Chalubinskiego 10, 50 368 Wroclaw, Poland
    Eur J Pharm Sci 21:421-7. 2004
    ..7-fold when length of the alkyl phenothiazine chain was enhanced by addition of the each next one (-CH(2)) group. Substitution of -H atom by -CF(3) group at position 2 of phenothiazine ring results in 3.5-fold increase in K(p) values...
  56. ncbi request reprint Alpha-hydroxyketones as inhibitors of urease
    Toru Tanaka
    Faculty of Pharmaceutical Sciences, Josai University, Sakado, Saitama 350 0295, Japan
    Bioorg Med Chem 12:501-5. 2004
    ..We have demonstrated for the first time that some alpha-hydroxyketone derivatives show urease inhibitory activity, possibly by binding to cysteinyl residues in the active site...
  57. ncbi request reprint Inhibitory action of a new proton pump inhibitor, trifluoromethyl ketone derivative, against the motility of clarithromycin-susceptible and-resistant Helicobacter pylori
    Gabriella Spengler
    Department of Medical Microbiology and Immunobiology, Albert Szent Gyorgyi Medical Centre, Faculty of Medicine, University of Szeged, Szeged, Hungary
    Int J Antimicrob Agents 23:631-3. 2004
    ..Based on the results, it is supposed that TF18 works as an uncoupler similar to the 'clutch' in a biological motor, in which counterclockwise rotation is more sensitive to the effect of TF18 than the clockwise rotation...
  58. ncbi request reprint Effect of antisense oligodeoxynucleotide for sepiapterin reductase on the viability of PC12 cells in the presence of exogenous carbonyl compounds
    Kengo Fujimoto
    Department of Biochemistry, Meikai University School of Dentistry, Sakado, 350 0283, Saitama, Japan
    Chem Biol Interact 143:583-6. 2003
    ..Thus, the SDR activity of SPR in PC12 cells may serve for detoxification of exogenous carbonyl compounds besides functioning as a specific enzyme for the formation of tetrahydrobiopterin...
  59. ncbi request reprint Presence of anionic phospholipids rules the membrane localization of phenothiazine type multidrug resistance modulator
    Olga Wesołowska
    Department of Biophysics, Wrocław Medical University, ul Chałubińskiego 10, 50 368 Wrocław, Poland
    Biophys Chem 109:399-412. 2004
    ..Behavior of equimolar PC:PS mixtures is similar to pure PS bilayers, while 2:1 or 1:2 (mole:mole) PC:PS mixtures resemble pure PC ones...
  60. ncbi request reprint Phenothiazine maleates stimulate MRP1 transport activity in human erythrocytes
    Olga Wesołowska
    Department of Biophysics, Wrocław Medical University, ul Chałubińskiego 10, 50 368 Wrocław, Poland
    Biochim Biophys Acta 1720:52-8. 2005
    ..We conclude that phenothiazine maleates probably exert their stimulatory effect on MRP1 by direct interaction with the protein at the site different from the substrate binding site...
  61. ncbi request reprint Urease inhibitory activity of simple alpha,beta-unsaturated ketones
    Toru Tanaka
    Faculty of Pharmaceutical Sciences, Josai University, Sakado, Saitama 350 0295, Japan
    Life Sci 73:2985-90. 2003
    ..These data suggest that alpha,beta-unsaturated ketones inhibited the urease activity, possibly by a Michael-like addition of a protein SH group to the double bond of the alpha,beta-unsaturated carbonyl group...
  62. ncbi request reprint Cytotoxic 5-aryl-1-(4-nitrophenyl)-3-oxo-1,4-pentadienes mounted on alicyclic scaffolds
    Umashankar Das
    College of Pharmacy and Nutrition, University of Saskatchewan, 110 Science Crescent, Saskatoon, Saskatchewan S7N 5C9, Canada
    Eur J Med Chem 41:577-85. 2006
    ..The modes of action of representative compounds include the induction of apoptosis while some compounds weakly inhibited tubulin polymerisation and human N-myristoyltransferase...
  63. ncbi request reprint Antimicrobial activity of N-acylphenothiazines and their influence on lipid model membranes and erythrocyte membranes
    Noboru Motohashi
    Meiji Pharmaceutical University, Kiyose, Tokyo, Japan
    Arzneimittelforschung 53:590-9. 2003
    ..Above results show that phenothiazine maleates were generally more effective than other phenothiazines used in this study...
  64. ncbi request reprint A study on the perturbation of model lipid membranes by phenoxazines
    Andrzej B Hendrich
    Department of Biophysics, Wrocław Medical University, Wrocław, Poland
    Bioorg Med Chem 14:5948-54. 2006
    ..These studies showed also that phenoxazine molecules are located close to the polar/apolar interface of bilayer. The results allow to conclude that phenoxazines rather weakly interact with lipid bilayers...