Enhancement of the Antiplasmodial Activity of Quassin by Transformation into a γ-Lactone
Тип публикации: Journal Article
Дата публикации: 2003-11-11
SCImago Q1
WOS Q2
БС1
SJR: 0.585
CiteScore: 6.3
Impact factor: 3.7
ISSN: 01633864, 15206025
PubMed ID:
14640524
Organic Chemistry
Drug Discovery
Pharmacology
Pharmaceutical Science
Molecular Medicine
Complementary and alternative medicine
Analytical Chemistry
Краткое описание
The naturally occurring bitter principle quassin (1) was converted chemically into the γ-lactone quassilactone (13) in an attempt to enhance its antiplasmodial activity. The in vitro antiplasmodial activity of 13 against Plasmodium falciparum (K1) (IC50 = 23 μM) was 40-fold greater than that of 1. However, one of the intermediates, compound 8, the 15β-hydroxy,16-O-m-chlorobenzoyl analogue of 1, was 506-fold more active than 1 against P. falciparum (IC50 = 1.8 μM) and only 3-fold less potent than chloroquine. In addition, 8 displayed the best cytotoxic/antiplasmodial ratio (112) of all of the compounds tested. In the course of this work a dimer, neoquassin ether (6), linked at C-16 was also prepared; 6 was found to have weak antiplasmodial activity (IC50 = 9.7 μM).
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ГОСТ
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Langat Thoruwa C. et al. Enhancement of the Antiplasmodial Activity of Quassin by Transformation into a γ-Lactone // Journal of Natural Products. 2003. Vol. 66. No. 11. pp. 1486-1489.
ГОСТ со всеми авторами (до 50)
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Langat Thoruwa C., Kirby G. C., PHILLIPSON J. D., Warhurst D. C., Watt R. A., Wright C. Enhancement of the Antiplasmodial Activity of Quassin by Transformation into a γ-Lactone // Journal of Natural Products. 2003. Vol. 66. No. 11. pp. 1486-1489.
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RIS
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TY - JOUR
DO - 10.1021/np030107a
UR - https://doi.org/10.1021/np030107a
TI - Enhancement of the Antiplasmodial Activity of Quassin by Transformation into a γ-Lactone
T2 - Journal of Natural Products
AU - Langat Thoruwa, Caroline
AU - Kirby, Geoffrey C
AU - PHILLIPSON, J. DAVID
AU - Warhurst, David C.
AU - Watt, Robert A
AU - Wright, Colin
PY - 2003
DA - 2003/11/11
PB - American Chemical Society (ACS)
SP - 1486-1489
IS - 11
VL - 66
PMID - 14640524
SN - 0163-3864
SN - 1520-6025
ER -
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BibTex (до 50 авторов)
Скопировать
@article{2003_Langat Thoruwa,
author = {Caroline Langat Thoruwa and Geoffrey C Kirby and J. DAVID PHILLIPSON and David C. Warhurst and Robert A Watt and Colin Wright},
title = {Enhancement of the Antiplasmodial Activity of Quassin by Transformation into a γ-Lactone},
journal = {Journal of Natural Products},
year = {2003},
volume = {66},
publisher = {American Chemical Society (ACS)},
month = {nov},
url = {https://doi.org/10.1021/np030107a},
number = {11},
pages = {1486--1489},
doi = {10.1021/np030107a}
}
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MLA
Скопировать
Langat Thoruwa, Caroline, et al. “Enhancement of the Antiplasmodial Activity of Quassin by Transformation into a γ-Lactone.” Journal of Natural Products, vol. 66, no. 11, Nov. 2003, pp. 1486-1489. https://doi.org/10.1021/np030107a.
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