抗肿瘤分子靶向抑制剂

Many past antitumor agents have predominately operated as non-specific cytotoxic tubulin inhibitors that, while successful have suffered from numerous drawbacks stemming from this non-specificity.¹⁾ Modern antitumor agents such as imatinib [I0906]²⁾ and regorafenib [R0142]³⁾ sought to improve upon these limitations by functioning as targeted kinase inhibitors and have improved side effect profiles and pose less hazards than tubulin inhibitors. Thalidomide [T2524] and pomalidomide [P2074]⁴⁾ have recently been shown to posess antitumor activities through its vascular endothelial growth factor (VEGF) inhibition. TCI provides high quality pharmaceutical reagents for investigate research and biomedical applications.

References

• 1) Targeted anti-mitotic therapies: can we improve on tubulin agents?
  • J. R. Jackson, D. R. Patrick, M. M. Dar, P. S. Huang, Nat. Rev. Cancer 2007, 7, 107.
• 2) Glivec (STI571, imatinib), a rationally developed, targeted anticancer drug
  • R. Capdeville, E. Buchdunger, J. Zimmermann, A. Matter, Nat. Rev. Drug Discovery 2002, 1, 493.
• 3) Regorafenib for cancer
  • D. Strumberg, B. Schultheis, Expert Opin. Invest. Drugs 2012, 21, 879.
• 4) The evolution of thalidomide and its IMiD derivatives as anticancer agents
  • J. B. Bartlett, K. Dredge, A. G. Dalgleish, Nat. Rev. Cancer 2004, 4, 314.

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