RRC ID 1149
著者 Komatsu K, Tsuda M, Tanaka Y, Mikami Y, Kobayashi J.
タイトル SAR studies of brasilicardin A for immunosuppressive and cytotoxic activities.
ジャーナル Bioorg Med Chem
Abstract Eleven derivatives (5-13, 15, and 16) of an immunosuppressive and cytotoxic tricyclic terpenoid, brasilicardin A (1), were prepared and assayed for inhibitory effects to the mouse mixed lymphocyte reaction (MLR) and seven human tumor cell lines. The 17N-methyl form (8) of 1 showed the most potent immunosuppressive activity in mouse MLR, while induction of more bulky group for N-17 resulted in significant decrease of the activity. Compound 8 also showed potent cytotoxic activity against DLD-1, Lu-65, A549, K562, and MOLT-4 cells, while the benzyl ester (13) of 1 exhibited potent cytotoxicity against K562, MOLT-4, and jarkat leukemia cell lines. The 17N-acetyl derivative (11) of 1 selectively inhibited the cell growth of DLD-1 cells. The methyl ester (5) of 1 showed potent cytotoxic activity against K562, MOLT-4, and Ball-1 cell lines, the last of which was resistant to 1, 8, and 13.
巻・号 13(5)
ページ 1507-13
公開日 2005-3-1
DOI 10.1016/j.bmc.2004.12.029
PII S0968-0896(04)01013-2
PMID 15698766
MeSH Aminoglycosides / chemistry* Aminoglycosides / pharmacology* Antineoplastic Agents / chemistry* Antineoplastic Agents / pharmacology* Cell Line, Tumor Drug Screening Assays, Antitumor Humans Magnetic Resonance Spectroscopy Spectrometry, Mass, Electrospray Ionization Structure-Activity Relationship
IF 3.073
引用数 13
WOS 分野 CHEMISTRY, ORGANIC CHEMISTRY, MEDICINAL BIOCHEMISTRY & MOLECULAR BIOLOGY
リソース情報
病原微生物