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Synthesis, inhibition of NO production and antiproliferative activities of some indole derivatives.
J Enzyme Inhib Med Chem. 2009 Oct; 24(5):1148-53.JE

Abstract

The synthesis and the biological evaluation of pyrano[3,2-e]indoles and their reaction intermediates are described. The compounds prepared were evaluated for their inhibition of NO production, antioxidant activity and also for their ability to inhibit in vitro the growth of four human tumor cell lines: large lung carcinoma (COR-L23), alveolar basal epithelial carcinoma (A549), amelanotic melanoma (C32) and melanoma (A375). The two reaction intermediates, 5a and 5b, showed the highest inhibition of NO production in murine monocytic macrophage (IC(50) = 1.1 microM and IC(50) = 2.3 microM respectively). Compound 5a was the most active against melanotic melanoma (IC(50) = 11.8 microM) while the other compounds exhibited weak cytotoxicity with IC(50) values >50 microM on all cell lines.

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Authors+Show Affiliations

Sinicropi MS
University of Calabria, Department of Pharmaceutical Sciences, 87036 Arcavacata di Rende (CS), Italy.
Caruso A
No affiliation info available
Conforti F
No affiliation info available
Marrelli M
No affiliation info available
El Kashef H
No affiliation info available
Lancelot JC
No affiliation info available
Rault S
No affiliation info available
Statti GA
No affiliation info available
Menichini F
No affiliation info available

MeSH

AnimalsAntineoplastic AgentsCell Line, TumorCell ProliferationHumansIndolesInhibitory Concentration 50MiceMolecular StructureNitric OxidePyrans

Pub Type(s)

Journal Article

Language

eng

PubMed ID

19555184

Citation

Sinicropi, Maria Stefania, et al. "Synthesis, Inhibition of NO Production and Antiproliferative Activities of some Indole Derivatives." Journal of Enzyme Inhibition and Medicinal Chemistry, vol. 24, no. 5, 2009, pp. 1148-53.
Sinicropi MS, Caruso A, Conforti F, et al. Synthesis, inhibition of NO production and antiproliferative activities of some indole derivatives. J Enzyme Inhib Med Chem. 2009;24(5):1148-53.
Sinicropi, M. S., Caruso, A., Conforti, F., Marrelli, M., El Kashef, H., Lancelot, J. C., Rault, S., Statti, G. A., & Menichini, F. (2009). Synthesis, inhibition of NO production and antiproliferative activities of some indole derivatives. Journal of Enzyme Inhibition and Medicinal Chemistry, 24(5), 1148-53. https://doi.org/10.1080/14756360802693890
Sinicropi MS, et al. Synthesis, Inhibition of NO Production and Antiproliferative Activities of some Indole Derivatives. J Enzyme Inhib Med Chem. 2009;24(5):1148-53. PubMed PMID: 19555184.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis, inhibition of NO production and antiproliferative activities of some indole derivatives. AU - Sinicropi,Maria Stefania, AU - Caruso,Anna, AU - Conforti,Filomena, AU - Marrelli,Mariangela, AU - El Kashef,Hussein, AU - Lancelot,Jean-charles, AU - Rault,Sylvain, AU - Statti,Giancarlo A, AU - Menichini,Francesco, PY - 2009/6/27/entrez PY - 2009/6/27/pubmed PY - 2010/2/26/medline SP - 1148 EP - 53 JF - Journal of enzyme inhibition and medicinal chemistry JO - J Enzyme Inhib Med Chem VL - 24 IS - 5 N2 - The synthesis and the biological evaluation of pyrano[3,2-e]indoles and their reaction intermediates are described. The compounds prepared were evaluated for their inhibition of NO production, antioxidant activity and also for their ability to inhibit in vitro the growth of four human tumor cell lines: large lung carcinoma (COR-L23), alveolar basal epithelial carcinoma (A549), amelanotic melanoma (C32) and melanoma (A375). The two reaction intermediates, 5a and 5b, showed the highest inhibition of NO production in murine monocytic macrophage (IC(50) = 1.1 microM and IC(50) = 2.3 microM respectively). Compound 5a was the most active against melanotic melanoma (IC(50) = 11.8 microM) while the other compounds exhibited weak cytotoxicity with IC(50) values >50 microM on all cell lines. SN - 1475-6374 UR - https://www.unboundmedicine.com/medline/citation/19555184/Synthesis_inhibition_of_NO_production_and_antiproliferative_activities_of_some_indole_derivatives_ L2 - https://www.tandfonline.com/doi/full/10.1080/14756360802693890 DB - PRIME DP - Unbound Medicine ER -