Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Design, Synthesis and Cytotoxicity of Chalcone Analogs Derived from 2-Phenylimino-3-phenylthiazolidin-4-one

Author(s): Vijay Satam, Ravi Kumar Bandi, Ajaya Kumar Behera, Bijay Kumar Mishra, Olivia Brockway, Samuel Tzou, Matthias Zeller, Moses Lee, Hari Pati.

Abstract:

Eleven novel chalcone analogs having a 2-phenylimino-3-phenylthiazolidin-4-one core structure were designed, synthesized and investigated for cytotoxicity against murine B16 and L1210 cancer cells. Single crystal X-ray structure analyses confirmed that these chalcone analogs adopt a Z-geometry about the alkene bond. One of the compounds, 3j, which possesses a 2-chloro-5-bromo substitution in the phenyl moiety, showed moderate cytotoxicity against murine (B16) and human melanoma (MDA-MB-435) cell lines with an IC50 value of 57 and 12 µ M, respectively. At 30 µ M, compound 3j had virtually no effects on the microtubules in A10 cells.

Keywords: Chalcones, 2-Phenylimino-3-phenylthiazolidin-4-one, Cytotoxicity, Tubulin, murine (B16), melanoma, Single crystal X-ray structure analyses, antimalarial, Thiazolidinone, antischistosomal agents, phenylimine substituents, S. epidermidis, MTT assay, antimitotic agents

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Article Details

VOLUME: 8
ISSUE: 8
Year: 2011
Page: [704 - 708]
Pages: 5
DOI: 10.2174/157018011796576033
Price: $58