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KMID : 0043320080310030300
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Archives of Pharmacal Research
2008 Volume.31 No. 3 p.300 ~ p.304
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Synthesis of DAAS Derivatives and Their Enhancement of HL-60 Leukemia Cell Differentiation
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Kim Seung-Hyun
Chung Sun-Young
Kim Young-Wall
Kim Tae-Sung
Choi Bo-Gil
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Abstract
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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.
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KEYWORD
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DAAS, Santonin, Leukemia cell differentiation, ATRA
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