Abstract
Artemisinin, the first and last naturally occurring 1, 2, 4-trioxane originated from Artemisia annua, L. and its derivatives are a potent class of antimalarial drugs. The clinical efficacy of these drugs is characterized by an almost immediate onset and rapid reduction of parasitemia, and it is high in such areas as well where multidrug-resistance is rampant. Furthermore, artemisinin and many of its analog possess not only antiparasitic effect against Plasmodium falciparum, Schistosoma japonicum and Clonorchis sinensi but also immuno-modulation effects, and antitumor activities. This review covers the chemistry of artemisinin including synthesis of acetal-, non acetaltype C-12 analogs, C-11- and C-13 derivatives from artemisitene, ring-contracted derivatives, dimers, and trimers. Modes of biological action of artemisinin - derived analogs are also reviewed. The main objective of this article is to review the literatures of recent progress taken place in chemistry, mode of biological actions of artemisinin, and its derivatives as antimalarial and antitumor agents during the last three years (1999-2001).
Keywords: artemisinin, deoxoartemisinin, deoxoartemisitene, antimalarial activity, antitumor activity, plasmodium falciparum, mode of action
Current Medicinal Chemistry
Title: Recent Advances in Artemisinin and Its Derivatives as Antimalarial and Antitumor Agents
Volume: 11 Issue: 10
Author(s): Mankil Jung, Kyunghoon Lee, Hanjo Kim and Moonsoo Park
Affiliation:
Keywords: artemisinin, deoxoartemisinin, deoxoartemisitene, antimalarial activity, antitumor activity, plasmodium falciparum, mode of action
Abstract: Artemisinin, the first and last naturally occurring 1, 2, 4-trioxane originated from Artemisia annua, L. and its derivatives are a potent class of antimalarial drugs. The clinical efficacy of these drugs is characterized by an almost immediate onset and rapid reduction of parasitemia, and it is high in such areas as well where multidrug-resistance is rampant. Furthermore, artemisinin and many of its analog possess not only antiparasitic effect against Plasmodium falciparum, Schistosoma japonicum and Clonorchis sinensi but also immuno-modulation effects, and antitumor activities. This review covers the chemistry of artemisinin including synthesis of acetal-, non acetaltype C-12 analogs, C-11- and C-13 derivatives from artemisitene, ring-contracted derivatives, dimers, and trimers. Modes of biological action of artemisinin - derived analogs are also reviewed. The main objective of this article is to review the literatures of recent progress taken place in chemistry, mode of biological actions of artemisinin, and its derivatives as antimalarial and antitumor agents during the last three years (1999-2001).
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Cite this article as:
Jung Mankil, Lee Kyunghoon, Kim Hanjo and Park Moonsoo, Recent Advances in Artemisinin and Its Derivatives as Antimalarial and Antitumor Agents, Current Medicinal Chemistry 2004; 11 (10) . https://dx.doi.org/10.2174/0929867043365233
DOI https://dx.doi.org/10.2174/0929867043365233 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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