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Acetal Derivative

The Experts below are selected from a list of 78 Experts worldwide ranked by ideXlab platform

Bo Gil Choi – 1st expert on this subject based on the ideXlab platform

  • Synthesis of C
    _6-epimer Derivatives of diacetoxy Acetal Derivative of santonin and their inducing effects on HL-60 leukemia cell differentiation
    Archives of Pharmacal Research, 2011
    Co-Authors: Sin Ho Kweon, Joon Hee Hong, Bo Gil Choi

    Abstract:

    Induction of differentiation is a new and promising approach to leukemia therapy, well illustrated by the treatment of acute promyelocytic leukemia with 1,25-dihydroxyvitamin D_3 [1,25-(OH)_2D_3] or all- trans retinoic acid (ATRA). Using combination of either 1,25-(OH)_2D_3 or ATRA and chemotherapy, adverse effects 1,25-(OH)_2D_3 or ATRA such as hypercalcemic effects have decreased, and long-term survival has improved. In a previous study, we demonstrated that santonin could be chemically modified into a diacetoxy Acetal Derivative of santonin with strong differentiation-inducing activity. In this study, we further synthesized C_6-epimer Derivatives of diacetoxy Acetal Derivative of santonin and tested their effects on HL-60 cell differentiation. Some of the C_6-epimer Derivatives themselves induced increases in cell differentiation. Especially, (11 S )-3,3-(ethylenedioxy) eudesmano-13-ol-6β-acetate ( 7 ) was demonstrated to induce differentiation with larger than 80% of the cells attaining a differentiated phenotype. Importantly, 7 strongly enhanced differentiation of HL-60 cells in a dose-dependent manner when combined with either low doses of 1,25-(OH)_2D_3 or ATRA. The ability to enhance the differentiation potential of 1,25-(OH)_2D_3 or ATRA by 7 may improve outcomes in the therapy of acute promyelocytic leukemia.

  • Synthesis of DAAS Derivatives and their enhancement of HL-60 leukemia cell differentiation
    Archives of Pharmacal Research, 2008
    Co-Authors: Sun Young Chung, Bo Gil Choi

    Abstract:

    DAAS is the diacetoxy Acetal Derivative of a-santonin and induces HL-60 cell differentiation into granulocytes. In this report, we investigated the structure-activity relationship (SAR) of DAAS Derivatives in the differentiation of human HL-60 leukemia cells. Although its Derivatives themselves had less effect on HL-60 cell differentiation than DAAS, the monoacetyl Derivative, 2 , mainly induced HL-60 cell differentiation. Moreover, compound 2 synergistically enhanced all- trans retinoic acid (ATRA)-induced HL-60 cell differentiation when combined with 50 nM ATRA, a well-known differentiation inducer. This enhancing effect is similar to that of DAAS in ATRA-induced differentiation.

Sun Young Chung – 2nd expert on this subject based on the ideXlab platform

  • Synthesis of DAAS Derivatives and their enhancement of HL-60 leukemia cell differentiation
    Archives of Pharmacal Research, 2008
    Co-Authors: Sun Young Chung, Bo Gil Choi

    Abstract:

    DAAS is the diacetoxy Acetal Derivative of a-santonin and induces HL-60 cell differentiation into granulocytes. In this report, we investigated the structure-activity relationship (SAR) of DAAS Derivatives in the differentiation of human HL-60 leukemia cells. Although its Derivatives themselves had less effect on HL-60 cell differentiation than DAAS, the monoacetyl Derivative, 2 , mainly induced HL-60 cell differentiation. Moreover, compound 2 synergistically enhanced all- trans retinoic acid (ATRA)-induced HL-60 cell differentiation when combined with 50 nM ATRA, a well-known differentiation inducer. This enhancing effect is similar to that of DAAS in ATRA-induced differentiation.

Sin Ho Kweon – 3rd expert on this subject based on the ideXlab platform

  • Synthesis of C
    _6-epimer Derivatives of diacetoxy Acetal Derivative of santonin and their inducing effects on HL-60 leukemia cell differentiation
    Archives of Pharmacal Research, 2011
    Co-Authors: Sin Ho Kweon, Joon Hee Hong, Bo Gil Choi

    Abstract:

    Induction of differentiation is a new and promising approach to leukemia therapy, well illustrated by the treatment of acute promyelocytic leukemia with 1,25-dihydroxyvitamin D_3 [1,25-(OH)_2D_3] or all- trans retinoic acid (ATRA). Using combination of either 1,25-(OH)_2D_3 or ATRA and chemotherapy, adverse effects 1,25-(OH)_2D_3 or ATRA such as hypercalcemic effects have decreased, and long-term survival has improved. In a previous study, we demonstrated that santonin could be chemically modified into a diacetoxy Acetal Derivative of santonin with strong differentiation-inducing activity. In this study, we further synthesized C_6-epimer Derivatives of diacetoxy Acetal Derivative of santonin and tested their effects on HL-60 cell differentiation. Some of the C_6-epimer Derivatives themselves induced increases in cell differentiation. Especially, (11 S )-3,3-(ethylenedioxy) eudesmano-13-ol-6β-acetate ( 7 ) was demonstrated to induce differentiation with larger than 80% of the cells attaining a differentiated phenotype. Importantly, 7 strongly enhanced differentiation of HL-60 cells in a dose-dependent manner when combined with either low doses of 1,25-(OH)_2D_3 or ATRA. The ability to enhance the differentiation potential of 1,25-(OH)_2D_3 or ATRA by 7 may improve outcomes in the therapy of acute promyelocytic leukemia.