The synthesis of cyclic tetrapeptoid analogues of the antiprotozoal natural product apicidin.
PJ Murray;
M Kranz;
M Ladlow;
S Taylor;
F Berst;
AB Holmes;
KN Keavey;
A Jaxa-Chamiec;
PW Seale;
P Stead;
+4 more...
RJ Upton;
SL Croft
;
W Clegg;
MR Elsegood;
(2001)
The synthesis of cyclic tetrapeptoid analogues of the antiprotozoal natural product apicidin.
Bioorganic & medicinal chemistry letters, 11 (6).
pp. 773-776.
ISSN 0960-894X
DOI: 10.1016/s0960-894x(01)00049-x
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.
Item Type | Article |
---|---|
Keywords | Histone deacetylase inhibitors, n-alkylation, chlamydocin, chromatin, peptides, trapoxin, linker, potent, agents, Animal, Parasitic Sensitivity Tests, Peptides, Cyclic, chemical synthesis, chemistry, pharmacology, Support, Non-U.S. Gov't, Trypanocidal Agents, chemical synthesis, chemistry, pharmacology, Trypanosoma brucei brucei, drug effects |
ISI | 167571100006 |
ORCID: https://orcid.org/0000-0002-3902-8006