Discovery of a potent tubulin polymerization inhibitor: Synthesis and evaluation of water-soluble prodrugs of benzophenone analog

Synthesis and evaluation of various amino acid prodrugs of 1 led to the discovery of 3· HCl (R = ( S)-isopropyl) which was shown to have potent antitumor efficacy in mouse xenografts. Pharmacokinetic study in rats was also described. Prodrugs have proven to be very useful in enhancing aqueous solubi...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-11, Vol.20 (21), p.6327-6330
Hauptverfasser:	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
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antineoplastic agents Antineoplastic Agents - chemical synthesis Antineoplastic Agents - pharmacology Antitumor activity Aqueous solubility Benzophenones - chemical synthesis Benzophenones - pharmacokinetics Benzophenones - pharmacology Biological and medical sciences Cell Proliferation - drug effects General aspects HL-60 Cells Humans Inhibitor Injections, Intravenous Male Medical sciences Mice Mice, Inbred BALB C Pharmacology. Drug treatments Prodrug Prodrugs - chemical synthesis Prodrugs - chemistry Rats Rats, Sprague-Dawley Solubility Tubulin Tubulin - biosynthesis Tubulin Modulators - chemical synthesis Tubulin Modulators - pharmacokinetics Tubulin Modulators - pharmacology Water Xenograft Model Antitumor Assays
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