Synthesis of DAAS derivatives and their enhancement of HL-60 leukemia cell differentiation.
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.
Kim
Seung Hyun
SH
School of Life Sciences and Biotechnology, Korea University, Seoul 136-701, Korea.
Chung
Sun Young
SY
Kim
Young Wall
YW
Kim
Tae Sung
TS
Choi
Bo Gil
BG
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D002454:Cell Differentiation / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D004357:Drug Synergism; D018922:HL-60 Cells; D006801:Humans; D007938:Leukemia / Q000188:drug therapy* / Q000473:pathology; D015394:Molecular Structure; D012500:Santonin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use; D013329:Structure-Activity Relationship; D014212:Tretinoin / Q000494:pharmacology
C511609:3,3-(ethylenedioxy)-eudesmano-13,6-diacetate; D000970:Antineoplastic Agents; D012500:Santonin; D014212:Tretinoin