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Synthesis and evaluation of anti-plasmodial and cytotoxic activities of epoxyazadiradione derivatives.
- Source :
-
European journal of medicinal chemistry [Eur J Med Chem] 2017 Jul 07; Vol. 134, pp. 242-257. Date of Electronic Publication: 2017 Apr 13. - Publication Year :
- 2017
-
Abstract
- Epoxyazadiradione (1), a major compound derived from Neem oil, showed modest anti-plasmodial activity against CQ-resistant and CQ-sensitive strains of the most virulent human malaria parasite P. falciparum. A series of analogues were synthesized by modification of the key structural moieties of this high yield natural product. Out of the library of all compounds tested, compounds 3c and 3g have showed modest anti-plasmodial activity against CQ-sensitive (IC <subscript>50</subscript> 2.8 ± 0.29 μM and 1.5 ± 0.01 μM) and CQ-resistant strains (IC <subscript>50</subscript> 1.3 ± 1.08 μM and 1.2 ± 0.14), while compounds 3k, 3l and 3m showed modest activity against CQ-sensitive strain of P. falciparum with IC <subscript>50</subscript> values of 2.3 ± 0.4 μM, 2.9 ± 0.1 μM and 1.7 ± 0.06 μM, respectively. Additionally, cytotoxic properties of these derivatives against SIHA, PANC 1, MDA-MB-231, and IMR-3 cancer cell lines were also studied and the results indicated that low cytotoxic potentials of all the derivatives which indicating the high selectivity index of the compounds.<br /> (Copyright © 2017 Elsevier Masson SAS. All rights reserved.)
- Subjects :
- Animals
Antimalarials chemical synthesis
Antimalarials isolation & purification
Antineoplastic Agents chemical synthesis
Antineoplastic Agents isolation & purification
Cell Line, Tumor
Cell Proliferation drug effects
Humans
Limonins chemical synthesis
Limonins isolation & purification
Malaria drug therapy
Malaria, Falciparum drug therapy
Mice
Mice, Inbred BALB C
Neoplasms drug therapy
Plasmodium berghei drug effects
Plasmodium falciparum drug effects
Antimalarials chemistry
Antimalarials pharmacology
Antineoplastic Agents chemistry
Antineoplastic Agents pharmacology
Azadirachta chemistry
Limonins chemistry
Limonins pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1768-3254
- Volume :
- 134
- Database :
- MEDLINE
- Journal :
- European journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 28419927
- Full Text :
- https://doi.org/10.1016/j.ejmech.2017.04.016