Synthesis and evaluation of potential complement inhibitory semisynthetic analogs of oleanolic acid

A number of semisynthetic analogs of oleanolic acid have been synthesized and tested for their complement inhibitory, cytotoxic and apoptotic activities. Among these, compounds 10 and 17 exhibited complement inhibitory potency superior to oleanolic acid. Both have also shown a moderate improvement i...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1999-07, Vol.9 (14), p.1889-1894
Main Authors: Assefa, Haregewein, Nimrod, Alison, Walker, Larry, Sindelar, Robert
Format: Article
Language:English
Subjects:
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Apoptosis - drug effects
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
Complement Inactivator Proteins - chemical synthesis
Complement Inactivator Proteins - chemistry
Complement Inactivator Proteins - pharmacology
DNA Fragmentation
Drug Evaluation, Preclinical
Humans
Medical sciences
Melanoma - drug therapy
Oleanolic Acid - analogs & derivatives
Oleanolic Acid - pharmacology
Pharmacology. Drug treatments
Structure-Activity Relationship
Tumor Cells, Cultured
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Summary:A number of semisynthetic analogs of oleanolic acid have been synthesized and tested for their complement inhibitory, cytotoxic and apoptotic activities. Among these, compounds 10 and 17 exhibited complement inhibitory potency superior to oleanolic acid. Both have also shown a moderate improvement in in vitro therapeutic index (T.I.). A number of semisynthetic analogs of oleanolic acid have been synthesized and tested for their complement inhibitory, cytotoxic and apoptotic activities.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(99)00314-5