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 significantly less potent than the natural products. The minimum structural pharmacophore has now been refined from eight to three possible structures.
McNulty
J
J
Institute of Molecular Catalysis, Department of Chemistry, Brock University, St. Catharines, Ontario, Canada. jmcnulty@chemiris.labs.brocku.ca
Mao
J
J
Gibe
R
R
Mo
R
R
Wolf
S
S
Pettit
G R
GR
Herald
D L
DL
Boyd
M R
MR
D047151:Amaryllidaceae Alkaloids; D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020128:Inhibitory Concentration 50; D007546:Isoquinolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051379:Mice; D008958:Models, Molecular; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured / Q000187:drug effects
D047151:Amaryllidaceae Alkaloids; D000972:Antineoplastic Agents, Phytogenic; D007546:Isoquinolines; C044997:pancratistatin