Studies directed towards the refinement of the pancratistatin cytotoxic pharmacophore

Two deoxy-analogues of the anticancer/antiviral agent pancratistatin containing functionality complementary to the minimum structural pharmacophore were synthesized and subjected to anticancer screening. One of the analogues exhibited selective inhibition of certain tumor cell lines but was signific...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2001-01, Vol.11 (2), p.169-172
Main Authors: MCNULTY, James, MAO, Justin, GIBE, Romelo, MO, Ruowei, WOLF, Sonja, PETTIT, George R, HERALD, Delbert L, BOYD, Michael R
Format: Article
Language:English
Subjects:
Amaryllidaceae Alkaloids
Animals
Antineoplastic agents
Antineoplastic Agents, Phytogenic - chemical synthesis
Antineoplastic Agents, Phytogenic - chemistry
Antineoplastic Agents, Phytogenic - pharmacology
Biological and medical sciences
Cell Division - drug effects
Drug Screening Assays, Antitumor
General aspects
Humans
Inhibitory Concentration 50
Isoquinolines - chemical synthesis
Isoquinolines - chemistry
Isoquinolines - pharmacology
Medical sciences
Mice
Models, Molecular
Pharmacology. Drug treatments
Structure-Activity Relationship
Tumor Cells, Cultured - drug effects
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Summary:Two deoxy-analogues of the anticancer/antiviral agent pancratistatin containing functionality complementary to the minimum structural pharmacophore were synthesized and subjected to anticancer screening. One of the analogues exhibited selective inhibition of certain tumor cell lines but was significantly less potent than the natural products. The minimum structural pharmacophore has now been refined from eight to three possible structures.
ISSN:0960-894X
1464-3405
DOI:10.1016/s0960-894x(00)00614-4