Synthesis and biological activities of 2-amino-1-arylidenamino imidazoles as orally active anticancer agents

Wen Tai Li, Der Ren Hwang, Jen Shin Song, Ching Ping Chen, Jiunn Jye Chuu, Chih Bo Hu, Heng Liang Lin, Chen Lung Huang, Chiung Yi Huang, Huan Yi Tseng, Chu Chung Lin, Tung Wei Chen, Chi Hung Lin, Hsin Sheng Wang, Chien Chang Shen, Chung Ming Chang, Yu Sheng Chao, Chiung Tong Chen*

*Corresponding author for this work

Research output: Contribution to journalArticle

30 Scopus citations

Abstract

2-Amino-l-arylidenaminoimidazoles, a novel class of orally (po) active microtubule-destabilizing anticancer agents, were synthesized. The compounds were designed from a hit compound identified in a drug discovery platform by using cancer cell-based high throughput screening assay. Selective synthesized compounds exerted cell cytotoxicity against human cancer cells. The underlying mechanisms for the anticancer activity were demonstrated as interacting with the tubulins and inhibiting microtubule assembly, leading to proliferation inhibition and apoptosis induction in the human tumor cells. Furthermore, two compounds showed in vivo anticancer activities in both po and intravenously (iv) administered routes and prolonged the life spans of murine leukemic P388 cells-inoculated mice. These new po active antimitotic anticancer agents are to be further examined in preclinical studies and developed for clinical uses.

Original languageEnglish
Pages (from-to)2409-2417
Number of pages9
JournalJournal of Medicinal Chemistry
Volume53
Issue number6
DOIs
StatePublished - 25 Mar 2010

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