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

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

  • J Med Chem. 2010 Mar 25;53(6):2409-17. doi: 10.1021/jm901501s.
Wen-Tai Li 1,  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
Affiliations

Affiliation

  • 1 Division of Biotechnology and Pharmaceutical Research, National Health Research Institutes, 35 Keyan Road, Zhunan, Miaoli 35053, Taiwan, ROC.
PMID: 20170097 DOI: 10.1021/jm901501s
Abstract

2-Amino-1-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.

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