The synthesis of cyclic tetrapeptoid analogues of the antiprotozoal natural product apicidin.
A novel synthetic strategy is described which may be used to prepare analogues of the antimalarial, fungal metabolite apicidin. Compared to the natural product, one analogue shows potent and selective activity in vitro against the parasite Trypanosoma brucei and low mammalian cell toxicity.
Glaxo Wellcome Cambridge Chemistry Laboratory, UK.
P J
PJ
Murray
M
M
Kranz
M
M
Ladlow
S
S
Taylor
F
F
Berst
A B
AB
Holmes
K N
KN
Keavey
A
A
Jaxa-Chamiec
P W
PW
Seale
P
P
Stead
R J
RJ
Upton
S L
SL
Croft
W
W
Clegg
M R
MR
Elsegood
D000818:Animals; D021261:Parasitic Sensitivity Tests; D010456:Peptides, Cyclic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014344:Trypanocidal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014346:Trypanosoma brucei brucei / Q000187:drug effects
D010456:Peptides, Cyclic; D014344:Trypanocidal Agents; C102351:apicidin