Acetic acid, 2-nitrophenyl ester → 7-Ethyl-10-Hydroxycamptothecin

반응식

CC(OC1C([N+]([O-])=O)=CC=CC=1)=O.[CH3:14][CH2:15][C:16]1[C:25]2[CH2:26][N:27]3[C:32](=[O:33])[C:31]4[CH2:34][O:35][C:36]([C@:38]([OH:41])([CH2:39][CH3:40])[C:30]=4[CH:29]=[C:28]3[C:24]=2[N:23]=[C:22]2[C:17]=1[CH:18]=[C:19]([O:42]C(N1CCC(N3CCCCC3)CC1)=O)[CH:20]=[CH:21]2)=[O:37].C1N(CCO)CCN(CCS(O)(=O)=O)C1>>[CH3:14][CH2:15][C:16]1[C:25]2[CH2:26][N:27]3[C:32](=[O:33])[C:31]4[CH2:34][O:35][C:36]([C@:38]([OH:41])([CH2:39][CH3:40])[C:30]=4[CH:29]=[C:28]3[C:24]=2[N:23]=[C:22]2[C:17]=1[CH:18]=[C:19]([OH:42])[CH:20]=[CH:21]2)=[O:37]

참가 물질

반응물 3

HCID 11890Acetic acid, 2-nitrophenyl ester

HCID 238314-(2-Hydroxyethyl)-1-piperazineethanesulfonic acid

HCID 60838Irinotecan2회

생성물 1

HCID 1048427-Ethyl-10-Hydroxycamptothecin

실험 절차

CE activity was determined by the spectrophotometric method described above for rabbit CE samples using o-NPA as a substrate. In another assay, activation of CPT-11 was determined by incubating samples of hiCE with either 5 μM or 25 μM CPT-11 in a total volume of 200 μl of 50 mM Hepes pH 7.4 at 37° C. for up to 20 hours. Reactions were terminated by the addition of an equal volume of cold acidified methanol, followed by centrifugation at 100,000×g for 30 minutes. The levels of SN-38 produced in the reaction were quantitated by HPLC.