Enantioselective Synthesis and Complement Inhibitory Assay of A/B-Ring Partial Analogues of Oleanolic Acid

A series of oleanolic acid A/B-ring partial analogues was synthesized and tested for their complement inhibitory activity as well as cytotoxic properties. All target compounds and one intermediate exhibited moderate complement inhibitory potency. These compounds also showed cytotoxicity on malignant...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2001-07, Vol.11 (13), p.1619-1623
Main Authors: Assefa, Haregewein, Nimrod, Alison, Walker, Larry, Sindelar, Robert
Format: Article
Language:English
Subjects:
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Biological and medical sciences
Complement Inactivator Proteins - chemical synthesis
Complement Inactivator Proteins - pharmacology
Drug Screening Assays, Antitumor
General aspects
Humans
Medical sciences
Melanoma - pathology
Oleanolic Acid - chemical synthesis
Oleanolic Acid - chemistry
Oleanolic Acid - pharmacology
Pharmacology. Drug treatments
Stereoisomerism
Tumor Cells, Cultured
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Summary:A series of oleanolic acid A/B-ring partial analogues was synthesized and tested for their complement inhibitory activity as well as cytotoxic properties. All target compounds and one intermediate exhibited moderate complement inhibitory potency. These compounds also showed cytotoxicity on malignant melanoma cell line, SK-MEL. A series of oleanlic acid A/B-ring parital analogues ( 1 and 2) was synthesized and tested for their complement inhibitory activity as well as cytotoxic properties.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(01)00210-4