Design, Syntheses and Biological Evaluation of 3-Arylurea-5-Fluoroindolin-2-One Derivatives

Abstract:

Sixteen 3-arylurea-5-fluoroindolin-2-one derivatives were designed according to the principle of fragment based drug discovery and synthesized with 5-fluoroisatin as the starting material. The obtained structures were identified by 1H NMR, MS and elemental analysis. In vitro evaluation of antitumor bioactivity was performed by MTT method. Most of synthesized compounds showed antitumor activities, especially, activities of 6a, 6h, and 6j in tumor inhibition were better than others.

• Periodical: Advanced Materials Research (Volumes 634-638)
• Pages: 922-925
• DOI: https://doi.org/10.4028/www.scientific.net/AMR.634-638.922
• Online since: January 2013
• Authors: Zhao Yang, Zhi Xiang Wang, Zheng Fang, Kai Guo
• Keywords: 3-Arylurea-5-Fluoroindolin-2-One, Activity, Antitumor, Synthesis

References

[1] L. C. Cantley, K. R. Auger, C. Carpenter, B. Duckworth, A. Graziani, R. Kapeller and S. Soltoff: Cell. Vol. 64 (1991), P. 281

DOI: 10.1016/0092-8674(91)90639-g

[2] L. K. Shawver, K. E. Lipson, T. A. T. Fong, G. McMahon, G. D. Plowman and L. M. Strawn: Drug. Discovery. Today. Vol. 2 (1997), P. 50

DOI: 10.1016/s1359-6446(96)10053-2

[3] S. Madhusudan, T. S. Ganesan: Chin. Biochem. Vol. 37 (2004), P. 618

[4] C. R. Prakash and S. Raja: MiniI-Rev. Med. Chem. Vol. 12 (2012), P. 98

[5] L. Rongshi and A. S. Jeffrey: Kinase Inhibitor Drugs (Wiley & Sons Publications, New Jersey 2009)

[6] Arslan MA, Kutuk O, Basaga H: Curr Cancer Drug Targets. Vol. 6 (2006), P. 623.

[7] Paul A. Renhowe, Sabina Pecchi, Cynthia M. Shafer, Timothy D: J. Med. Chem. Vol. 52 (2009), P. 278