Document Detail

Synthetic indole and melatonin derivatives exhibit antimalarial activity on the cell cycle of the human malaria parasite Plasmodium falciparum.
MedLine Citation:
PMID:  24699367     Owner:  NLM     Status:  Publisher    
Discovering the mechanisms by which cell signaling controls the cell cycle of the human malaria parasite Plasmodium falciparum is fundamental to designing more effective antimalarials. To better understand the impacts of melatonin structure and function on the cell cycle of P. falciparum, we have synthesized two families of structurally-related melatonin compounds (7-11 and 12-16). All synthesized melatonin analogs were assayed in P. falciparum culture and their antimalarial activities were measured by flow cytometry. We have found that the chemical modification of the carboxamide group attached at C-3 position of the indole ring of melatonin (6) was crucial for the action of the indole-related compounds on the P. falciparum cell cycle. Among the melatonin derivatives, only the compounds 12, 13 and 14 were capable of inhibiting the P. falciparum growth in low micromolar IC50. These results open good perspectives for the development of new drugs with novel mechanisms of action.
Desirée C Schuck; Alessandro K Jordão; Myna Nakabashi; Anna C Cunha; Vitor F Ferreira; Célia R S Garcia
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2014-3-18
Journal Detail:
Title:  European journal of medicinal chemistry     Volume:  78C     ISSN:  1768-3254     ISO Abbreviation:  Eur J Med Chem     Publication Date:  2014 Mar 
Date Detail:
Created Date:  2014-4-4     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0420510     Medline TA:  Eur J Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  375-382     Citation Subset:  -    
Copyright Information:
Copyright © 2014 Elsevier Masson SAS. All rights reserved.
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