1240321-53-2Relevant academic research and scientific papers
Identification of CKD-516: A potent tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors
Lee, Jaekwang,Kim, Soo Jin,Choi, Hojin,Kim, Young Hoon,Lim, In Taek,Yang, Hyun-Mo,Lee, Chang Sik,Kang, Hee Ryong,Ahn, Soon Kil,Moon, Seung Kee,Kim, Dal-Hyun,Lee, Sungsook,Choi, Nam Song,Lee, Kyung Joo
experimental part, p. 6337 - 6354 (2010/10/21)
Tubulin polymerization inhibitors had emerged as one of promising anticancer therapeutics because of their dual mechanism of action, i.e. apoptosis by cell-cycle arrest and VDA, vascular disrupting agent. VDAs are believed to be more efficient, less toxic
Discovery of a potent tubulin polymerization inhibitor: Synthesis and evaluation of water-soluble prodrugs of benzophenone analog
Lee, Jaekwang,Bae, Suyeal,Lee, Seo-Hee,Choi, Hojin,Kim, Young Hoon,Kim, Soo Jin,Park, Gyu Tae,Moon, Seung Kee,Kim, Dal-Hyun,Lee, Sungsook,Ahn, Soon Kil,Choi, Nam Song,Lee, Kyung Joo
scheme or table, p. 6327 - 6330 (2010/12/18)
Prodrugs have proven to be very useful in enhancing aqueous solubility of sparingly water-soluble drugs, thereby increasing in vivo efficacy without a need of special excipients. In vitro and in vivo evaluations of a number of amino acid prodrugs of 1, a previously identified potent tubulin polymerization inhibitor and cytotoxic against various cancer cell lines led to the discovery of 3·HCl (l-valine attached) which is highly efficacious in mouse xenografts bearing human cancer. Pharmacokinetic analysis in rats revealed that compound 1 was released immediately upon administration of 3·HCl intravenously, with rapid clearance of 3·HCl indicating the effective cleavage of prodrug. Compound 3·HCl (CKD-516) has now been progressed to phase 1 clinical trial.
