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Synthesis and evaluation of some novel N-substituted rhodanines for their anticancer activity

Synthesis and evaluation of some novel N-substituted rhodanines for their anticancer activity Novel N-substituted rhodanines 2a–g were synthesized by conventional and microwave-assisted methods and tested for their anticancer activity. Structure–activity relationship of the synthesized rhodanine 2a–g as antiproliferative agents was investigated. The results revealed that all the seven compounds showed potent antiproliferative activity in a concentration-dependent manner on leukemic cell line K562. Among the tested compounds, 2b was found to be more potent when compared by trypan blue and MTT assay. IC50 values of 2b using trypan blue and MTT assay were found to be 11.1 and 20.3 µg/ml, respectively. A dose-dependent increase in the LDH release was also observed upon treatment with 2a–g. Cell cycle analysis revealed that 2b affects DNA replication and leads to accumulation of cells in G 0 and decline of G 2/M, G 1 and S phases which indicates apoptosis. The selective cytotoxic activity against human chronic myelogenous cell line (K562), via apoptosis, suggests that compound 2b is a promising scaffold for the development of novel anticancer drug. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Medicinal Chemistry Research Springer Journals

Synthesis and evaluation of some novel N-substituted rhodanines for their anticancer activity

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Publisher
Springer Journals
Copyright
Copyright © 2016 by Springer Science+Business Media New York
Subject
Biomedicine; Pharmacology/Toxicology; Biochemistry, general; Cell Biology
ISSN
1054-2523
eISSN
1554-8120
DOI
10.1007/s00044-016-1545-7
Publisher site
See Article on Publisher Site

Abstract

Novel N-substituted rhodanines 2a–g were synthesized by conventional and microwave-assisted methods and tested for their anticancer activity. Structure–activity relationship of the synthesized rhodanine 2a–g as antiproliferative agents was investigated. The results revealed that all the seven compounds showed potent antiproliferative activity in a concentration-dependent manner on leukemic cell line K562. Among the tested compounds, 2b was found to be more potent when compared by trypan blue and MTT assay. IC50 values of 2b using trypan blue and MTT assay were found to be 11.1 and 20.3 µg/ml, respectively. A dose-dependent increase in the LDH release was also observed upon treatment with 2a–g. Cell cycle analysis revealed that 2b affects DNA replication and leads to accumulation of cells in G 0 and decline of G 2/M, G 1 and S phases which indicates apoptosis. The selective cytotoxic activity against human chronic myelogenous cell line (K562), via apoptosis, suggests that compound 2b is a promising scaffold for the development of novel anticancer drug.

Journal

Medicinal Chemistry Research – Springer Journals

Published: Mar 3, 2016

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