@article{464f6c1da22745fbaa75330c64d8968f,
title = "Diverted total synthesis of falcitidin acyl tetrapeptides as new antimalarial leads",
abstract = "We report not only the convergent total synthesis of falcitidin, a natural inhibitor of falcipain-2 from myxobacterium Chitinophaga, but also its diversification into a new antimalarial class of N-acyl tetrapeptides (Acyl-His-Ile-Val-Pro-NH2). Despite the lack of whole-cell activity of falcitidin itself, our study led to the identification of a trifluoromethyl (CF3) analogue displaying sub-micromolar IC50 activity against Plasmodium falciparum 3D7 in a standard blood-cell assay, but only when N-tritylated on its histidine (imidazole) residue.",
keywords = "Antimalarial agents, Falcitidin, Natural products, Tetrapeptide, Trifluoromethyl",
author = "Kotturi, {Santosh R.} and Brinda Somanadhan and Ch'Ng, {Jun Hong} and Tan, {Kevin S.W.} and Butler, {Mark S.} and Lear, {Martin J.}",
note = "Funding Information: We thank the Ministry of Education of Singapore for initial funding (AcRF Tier-2 Grant T206B1112 ) and a Ph.D. graduate scholarship (to S.R.K.). We appreciate the help of Alvin Choong for initial antimalarial tests. Latterly, this work was supported by the National Medical Research Council (NMRC/1310/2011) of Singapore (to K.S.W.T., J.H.C. and M.J.L.). ",
year = "2014",
month = mar,
day = "12",
doi = "10.1016/j.tetlet.2014.02.008",
language = "English",
volume = "55",
pages = "1949--1951",
journal = "Tetrahedron Letters",
issn = "0040-4039",
publisher = "Elsevier Limited",
number = "11",
}