Design, synthesis and evaluation of novel rhodanine-containing sorafenib analogs as potential antitumor agents.

Abstract

A series of rhodanine-containing sorafenib analogs was designed, synthesized and evaluated for their in-vitro antitumor activity against three cancer cell lines (A549, H460 and HT29). Pharmacological data indicated that some of the target compounds possessed marked antiproliferative activity superior to the reference drug sorafenib, especially the most promising compound 7r (with the IC(50) value of 0.8, 1.3 and 2.8 µM against A549, H460 and HT29 cell lines, respectively). The activity was found to strongly depend on the substitution pattern of the rhodanine motif at C-5″ position. Results suggested that this series of compounds could serve as the bases for the development of novel antitumor agents.

• Authors: Wei Li, Xin Zhai, Zheng Zhong, Guangyue Li, Yongxiao Pu, Ping Gong
• Journal: Archiv der Pharmazie (Arch Pharm (Weinheim)) Vol. 344 Issue 6 Pg. 349-57 (Jun 2011) ISSN: 1521-4184 [Electronic] Germany
• PMID: 21433057 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Chemical References

• Antineoplastic Agents
• Benzenesulfonates
• Phenylurea Compounds
• Pyridines
• Niacinamide
• Rhodanine
• Sorafenib

Topics

• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
• Benzenesulfonates (chemical synthesis, chemistry, pharmacology)
• Cell Line, Tumor
• Cell Proliferation (drug effects)
• HT29 Cells
• Humans
• Inhibitory Concentration 50
• Neoplasms (drug therapy, pathology)
• Niacinamide (analogs & derivatives)
• Phenylurea Compounds
• Pyridines (chemical synthesis, chemistry, pharmacology)
• Rhodanine (chemistry)
• Sorafenib
• Structure-Activity Relationship