A 10-step, asymmetric synthesis of (S)-camptothecin
DL Comins, MF Baevsky, H Hong - Journal of the american …, 1992 - ACS Publications
DL Comins, MF Baevsky, H Hong
Journal of the american Chemical Society, 1992•ACS Publications(S)-Camptothecin (1), a pentacyclic alkaloid isolated from Camptotheca acuminata by Wall
and co-workersin 1966, con-tinues to be one of the most important lead compounds among
the anticancer natural products. 1 A number of promising analogs have been prepared that
show improved solubility, low overall toxicity, and impressive in vivo activity against certain
solid tu-mors. 2 Some of the more active derivatives include 9-amino-camptothecin2®(2),
10, 11-(methylenedioxyjcamptothecin2®· 3 (3), and (20S)-9-[(dimethylamino) methyl]-10 …
and co-workersin 1966, con-tinues to be one of the most important lead compounds among
the anticancer natural products. 1 A number of promising analogs have been prepared that
show improved solubility, low overall toxicity, and impressive in vivo activity against certain
solid tu-mors. 2 Some of the more active derivatives include 9-amino-camptothecin2®(2),
10, 11-(methylenedioxyjcamptothecin2®· 3 (3), and (20S)-9-[(dimethylamino) methyl]-10 …
(S)-Camptothecin (1), a pentacyclic alkaloid isolated from Camptotheca acuminata by Wall and co-workersin 1966, con-tinues to be one of the most important lead compounds among the anticancer natural products. 1 A number of promising analogs have been prepared that show improved solubility, low overall toxicity, and impressive in vivo activity against certain solid tu-mors. 2 Some of the more active derivatives include 9-amino-camptothecin2®(2), 10, 11-(methylenedioxyjcamptothecin2®· 3 (3), and (20S)-9-[(dimethylamino) methyl]-10-hydroxycamptothecin2b (4). Analog 4 is currently undergoing phase I clinical trials in cancer patients. The camptothecins’ mode of action has been
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