Synthesis of Novel G Factor or Chloroquine-Artemisinin Hybrids and Conjugates with Potent Antiplasmodial Activity.

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ID: 107709
2020
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Abstract
A series of novel hybrids of artemisinin (ART) with either a phytormone endoperoxide G factor analogue (GMeP) or chloroquine (CQ) and conjugates of the same compounds with the polyamines (PAs), spermidine (Spd), and homospermidine (Hsd) were synthesized and their antiplasmodial activity was evaluated using the CQ-resistant FcB1/Colombia strain. The ART-GMeP hybrid and compounds and which are conjugates of Spd and Hsd with two molecules of ART and one molecule of GMeP, were the most potent with IC values of 2.6, 8.4, and 10.6 nM, respectively. The same compounds also presented the highest selectivity indexes against the primary human fibroblast cell line AB943 ranging from 16 372 for the hybrid to 983 for the conjugate of Hsd.
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pepe2020synthesisacs Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Pepe, Dionissia A;Toumpa, Dimitra;André-Barrès, Christiane;Menendez, Christophe;Mouray, Elisabeth;Baltas, Michel;Grellier, Philippe;Papaioannou, Dionissios;Athanassopoulos, Constantinos M;
Journal ACS medicinal chemistry letters
Year 2020
DOI
10.1021/acsmedchemlett.9b00669
URL
Keywords
coronavirus hydroxychloroquine sudden death arrhythmia chloroquine covid-19 sars-cov-2 torsades de pointes

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