Skip to main content
padlock icon - secure page this page is secure

Acyl Thiourea Derivatives Containing Pyrazole Ring Selective Targeting of Human Aurora Kinases in Breast and Bone Cancer

Buy Article:

$68.00 + tax (Refund Policy)

Several oncogenic pathways may lead to cancer. Pharmaceutical research develops efficacious compounds to inhibit these pathways. Current inhibitor drugs may block several pathways simultaneously but cause adverse and side effects. Therefore, we designed novel acyl thiourea derivatives containing pyrazole ring to selectively inhibit a kinase dependent pathway in cancer. In this study, breast and bone cancer cells were employed to monitor this selectivity. Since metastatic breast cancer spreads to bone, MCF-7 along with epithelial (Saos-2) and fibroblast (MG-63) human bone cancer cell lines were used to observe inhibitory effects of the synthesized compounds. It has been reported that Estrogen receptor α (ER-α) and Aurora kinase A and B are involved in different pathways at breast and bone cancer mechanism. Synthesized novel inhibitors presented in this work effectively and selectively bind to Aurora kinase A and B but do not interact with ER-α however; a generic inhibitor PHA-739358 binds to all three enzymes. This improved binding mode of the novel inhibitors may be a useful therapeutic strategy for the treatment of breast and bone cancer approaches and provides potency to personalized medicine.
No References
No Citations
No Supplementary Data
No Article Media
No Metrics

Keywords: Aurora kinases; bone cancer; breast cancer; estrogen receptor alpha; pyrazoles

Document Type: Research Article

Publication date: March 1, 2015

More about this publication?
  • Letters in Drug Design & Discovery publishes original letters on all areas of rational drug design and discovery including medicinal chemistry, in-silico drug design, combinatorial chemistry, high-throughput screening, drug targets, and structure-activity relationships. The emphasis will be on publishing quality papers very rapidly. Letters will be processed rapidly by taking full advantage of Internet technology for both the submission and review of manuscripts. The journal is essential reading to all pharmaceutical scientists involved in research in drug design and discovery.
  • Editorial Board
  • Information for Authors
  • Subscribe to this Title
  • Ingenta Connect is not responsible for the content or availability of external websites
  • Access Key
  • Free content
  • Partial Free content
  • New content
  • Open access content
  • Partial Open access content
  • Subscribed content
  • Partial Subscribed content
  • Free trial content
Cookie Policy
Cookie Policy
Ingenta Connect website makes use of cookies so as to keep track of data that you have filled in. I am Happy with this Find out more