Synthesis of constrained ceramide analogs and their potent antileukemic activities.
Constrained ceramide analogs were designed and synthesized by binding terminal alcohol and amine of ceramide with additional carbonyl functional group as 3-acetyl (3), 3-propionyl (4), 3-benzoyl (5), and 3-hexadecanoyl-4-(1-hydroxyhexadec-2-enyl)-oxazolidin-2-ones (6). Compounds 4 and 5 showed potent antileukemic activities against human leukemia HL-60 cells with good correlation between cell death and DNA fragmentation.
Ha
Hyun-Joon
HJ
Department of Chemistry, Hankuk University of Foreign Studies, Yongin 449-791, Republic of Korea. hjha@hufs.ac.kr
Hong
Myeng Chan
MC
Ko
Seung Whan
SW
Kim
Yong Woo
YW
Lee
Won Koo
WK
Park
Jungchan
J
D017209:Apoptosis / Q000187:drug effects; D002518:Ceramides / Q000138:chemical synthesis* / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D004587:Electrophoresis, Agar Gel; D018922:HL-60 Cells; D006801:Humans; D007938:Leukemia / Q000473:pathology*
D002518:Ceramides