Synthesis and antimalarial evaluation of novel isocryptolepine derivatives
A series of mono- and di-substituted analogues of isocryptolepine have been synthesized and evaluated for in vitro antimalarial activity against chloroquine sensitive (3D7) and resistant (W2mef) Plasmodium falciparum and for cytotoxicity (3T3 cells). Di-halogenated compounds were the most potent der...
| Main Authors: | , , , , , , |
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| Format: | Journal Article |
| Published: |
Elsevier
2011
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| Online Access: | http://hdl.handle.net/20.500.11937/44272 |
| _version_ | 1848756952573673472 |
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| author | Whittell, Louise Batty, Kevin Wong, R. Bolitho, Erin Fox, Simon Davis, T. Murray, Paul |
| author_facet | Whittell, Louise Batty, Kevin Wong, R. Bolitho, Erin Fox, Simon Davis, T. Murray, Paul |
| author_sort | Whittell, Louise |
| building | Curtin Institutional Repository |
| collection | Online Access |
| description | A series of mono- and di-substituted analogues of isocryptolepine have been synthesized and evaluated for in vitro antimalarial activity against chloroquine sensitive (3D7) and resistant (W2mef) Plasmodium falciparum and for cytotoxicity (3T3 cells). Di-halogenated compounds were the most potent derivatives and 8-bromo-2-chloroisocryptolepine displayed the highest selectivity index (106; the ratio of cytotoxicity (IC50 = 9005 nM) to antimalarial activity (IC50 = 85 nM)). Our evaluation of novel isocryptolepine compounds has demonstrated that di-halogenated derivatives are promising antimalarial lead compounds. |
| first_indexed | 2025-11-14T09:20:22Z |
| format | Journal Article |
| id | curtin-20.500.11937-44272 |
| institution | Curtin University Malaysia |
| institution_category | Local University |
| last_indexed | 2025-11-14T09:20:22Z |
| publishDate | 2011 |
| publisher | Elsevier |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | curtin-20.500.11937-442722017-09-13T16:03:55Z Synthesis and antimalarial evaluation of novel isocryptolepine derivatives Whittell, Louise Batty, Kevin Wong, R. Bolitho, Erin Fox, Simon Davis, T. Murray, Paul A series of mono- and di-substituted analogues of isocryptolepine have been synthesized and evaluated for in vitro antimalarial activity against chloroquine sensitive (3D7) and resistant (W2mef) Plasmodium falciparum and for cytotoxicity (3T3 cells). Di-halogenated compounds were the most potent derivatives and 8-bromo-2-chloroisocryptolepine displayed the highest selectivity index (106; the ratio of cytotoxicity (IC50 = 9005 nM) to antimalarial activity (IC50 = 85 nM)). Our evaluation of novel isocryptolepine compounds has demonstrated that di-halogenated derivatives are promising antimalarial lead compounds. 2011 Journal Article http://hdl.handle.net/20.500.11937/44272 10.1016/j.bmc.2011.10.037 Elsevier restricted |
| spellingShingle | Whittell, Louise Batty, Kevin Wong, R. Bolitho, Erin Fox, Simon Davis, T. Murray, Paul Synthesis and antimalarial evaluation of novel isocryptolepine derivatives |
| title | Synthesis and antimalarial evaluation of novel isocryptolepine derivatives |
| title_full | Synthesis and antimalarial evaluation of novel isocryptolepine derivatives |
| title_fullStr | Synthesis and antimalarial evaluation of novel isocryptolepine derivatives |
| title_full_unstemmed | Synthesis and antimalarial evaluation of novel isocryptolepine derivatives |
| title_short | Synthesis and antimalarial evaluation of novel isocryptolepine derivatives |
| title_sort | synthesis and antimalarial evaluation of novel isocryptolepine derivatives |
| url | http://hdl.handle.net/20.500.11937/44272 |