| Literature DB >> 12502374 |
Erin Joseph1, Julie L Eiseman, Diana S Hamilton, Haibo Wang, Heekyung Tak, Zhebo Ding, Bruce Ganem, Donald J Creighton.
Abstract
The antitumor activity of 2-crotonyloxymethyl-2-cyclohexenone (COMC-6) is not the result of the GSH conjugate (GSMC-6) formed inside tumor cells, as the diethyl ester prodrug form of GSMC-6 displays little antitumor activity with B16 melanotic melanoma in vitro (IC(50) > 460 microM) versus COMC-6 (IC(50) 0.041 microM) and its five- and seven-membered ring homologues. Antitumor activity probably results from a reactive intermediate that forms during conjugation of the COMCs with intracellular GSH.Entities:
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Year: 2003 PMID： 12502374 DOI： 10.1021/jm0203027
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446