DELAMINOMYCINS, NOVEL EXTRACELLULAR MATRIX RECEPTOR ANTAGONIST: IV. STRUCTURE-ACTIVITY RELATIONSHIPS OF DELAMINOMYCINS AND DERIVATIVES

Delaminomycins A, B, C and their derivatives were prepared and investigated biological activities of them. Among these compounds, spiro compounds (A2, B2 and C2) showed stronger inhibitory activity than natural products (A1, B1 and C1) on B16 melanoma cells adhesion assay and Con A-induced prolifera...

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Bibliographic Details
Published in:Journal of antibiotics 1993/07/25, Vol.46(7), pp.1156-1162
Main Authors: UENO, MITSUHIRO, AMEMIYA, MASAHIDE, YAMAZAKI, KATSUHISA, IIJIMA, MASATOMI, OSONO, MICHIYO, SOMENO, TETSUYA, IINUMA, HIRONOBU, HAMADA, MASA, ISHIZUKA, MASAAKI, TAKEUCHI, TOMIO
Format: Article
Language:English
Subjects:
Animals
Antibiotics, Antineoplastic - pharmacology
Antineoplastic agents
Biological and medical sciences
Cell Adhesion - drug effects
Drug Screening Assays, Antitumor
General aspects
Immunosuppressive Agents - pharmacology
Lymphocyte Activation - drug effects
Lymphocyte Culture Test, Mixed
Medical sciences
Melanoma, Experimental - drug therapy
Mice
Microbial Sensitivity Tests
Pharmacology. Drug treatments
Pyrrolidinones - pharmacology
Structure-Activity Relationship
Tetrahydronaphthalenes - pharmacology
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Summary:Delaminomycins A, B, C and their derivatives were prepared and investigated biological activities of them. Among these compounds, spiro compounds (A2, B2 and C2) showed stronger inhibitory activity than natural products (A1, B1 and C1) on B16 melanoma cells adhesion assay and Con A-induced proliferation of murine splenic lymphocytes assay. In MLCR and antimicrobial assay, however, A1, B1 and C1 showed more potent inhibitory activity than spiro compounds (A2, B2 and C2). On the other hand, as to C-5' substituents of pyrrolidine ring, the order of inhibitory activity was R=OH>R=OCH3>R=H on Con A-induced proliferation of murine splenic lymphocytes assay. In MLCR and antimicrobial assay, however, the order of inhibitory activities were R=H>R=OCH3>R=OH. Inhibitory activities of A4 which was lacked pyrrolidine ring were reduced on B16 melanoma cells adhesion assay and on cytotoxicity against tumor cells in vitro in comparison with those of A1.
ISSN:0021-8820
1881-1469
DOI:10.7164/antibiotics.46.1156