The synthesis of cyclic tetrapeptoid analogues of the antiprotozoal natural product apicidin


Murray, PJ; Kranz, M; Ladlow, M; Taylor, S; Berst, F; Holmes, AB; Keavey, KN; Jaxa-Chamiec, A; Seale, PW; Stead, P; Upton, RJ; Croft, SL; Clegg, W; Elsegood, MRJ; (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: https://doi.org/10.1016/S0960-894X(01)00049-X

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Abstract

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. (C) 2001 Elsevier Science Ltd. All rights reserved.

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
Faculty and Department: Faculty of Infectious and Tropical Diseases > Dept of Immunology and Infection
PubMed ID: 11277517
Web of Science ID: 167571100006
URI: http://researchonline.lshtm.ac.uk/id/eprint/16562

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