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Molecules 2018, 23(11), 2878; https://doi.org/10.3390/molecules23112878

Anti-Leishmanial and Cytotoxic Activities of a Series of Maleimides: Synthesis, Biological Evaluation and Structure-Activity Relationship

1
Institute of Fermentation Engineering, College of Biotechnology and Bioengineering, Zhejiang University of Technology, 18# Chaowang Road, Hangzhou 310032, China
2
National Center for Natural Products Research, Research Institute of Pharmaceutical Sciences and Department of BioMolecular Sciences, School of Pharmacy, The University of Mississippi, University, MS 38677, USA
*
Author to whom correspondence should be addressed.
Academic Editors: Muhammad Ilias and Charles L. Cantrell
Received: 25 September 2018 / Revised: 18 October 2018 / Accepted: 31 October 2018 / Published: 5 November 2018
Full-Text   |   PDF [753 KB, uploaded 5 November 2018]   |  

Abstract

In the present study, 45 maleimides have been synthesized and evaluated for anti-leishmanial activities against L. donovani in vitro and cytotoxicity toward THP1 cells. All compounds exhibited obvious anti-leishmanial activities. Among the tested compounds, there were 10 maleimides with superior anti-leishmanial activities to standard drug amphotericin B, and 32 maleimides with superior anti-leishmanial activities to standard drug pentamidine, especially compounds 16 (IC50 < 0.0128 μg/mL) and 42 (IC50 < 0.0128 μg/mL), which showed extraordinary efficacy in an in vitro test and low cytotoxicities (CC50 > 10 μg/mL). The anti-leishmanial activities of 16 and 42 were 10 times better than that of amphotericin B. The structure and activity relationship (SAR) studies revealed that 3,4-non-substituted maleimides displayed the strongest anti-leishmanial activities compared to those for 3-methyl-maleimides and 3,4-dichloro-maleimides. 3,4-dichloro-maleimides were the least cytotoxic compared to 3-methyl-maleimides and 3,4-non-substituted maleimides. The results show that several of the reported compounds are promising leads for potential anti-leishmanial drug development. View Full-Text
Keywords: anti-leishmanial activity; Leishmania donovani; maleimides; cytotoxicity; SAR anti-leishmanial activity; Leishmania donovani; maleimides; cytotoxicity; SAR
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Fan, Y.; Lu, Y.; Chen, X.; Tekwani, B.; Li, X.-C.; Shen, Y. Anti-Leishmanial and Cytotoxic Activities of a Series of Maleimides: Synthesis, Biological Evaluation and Structure-Activity Relationship. Molecules 2018, 23, 2878.

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