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

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

Volume: 8 Issue: 8

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

Affiliation:

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

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.

Cite this article as:

Satam Vijay, Bandi Ravi Kumar, Behera Ajaya Kumar, Mishra Bijay Kumar, Brockway Olivia, Tzou Samuel, Zeller Matthias, Lee Moses and Pati Hari, Design, Synthesis and Cytotoxicity of Chalcone Analogs Derived from 2-Phenylimino-3-phenylthiazolidin-4-one, Letters in Drug Design & Discovery 2011; 8(8) . https://dx.doi.org/10.2174/157018011796576033