In:
ChemMedChem, Wiley, Vol. 3, No. 12 ( 2008-12-15), p. 1946-1955
Abstract:
A severe limitation in cancer therapy is the often insufficient differentiation between malign and benign tissue using known chemotherapeutics. One approach to decrease side effects is antibody‐directed enzyme prodrug therapy (ADEPT). We have developed new glycosidic prodrugs such as (−)‐(1 S )‐ 26 b based on the antibiotic (+)‐duocarmycin SA ((+)‐ 1 ) with a QIC 50 value of 3500 (QIC 50 =IC 50 of prodrug/IC 50 of prodrug+enzyme) and an IC 50 value for the corresponding drug (prodrug+enzyme) of 16 p M . The asymmetric synthesis of the precursor (−)‐(1 S )‐ 19 was performed by arylation of the enantiomerically pure epoxide (+)‐( S )‐ 29 (≥98 % ee ).
Type of Medium:
Online Resource
ISSN:
1860-7179
,
1860-7187
DOI:
10.1002/cmdc.200800250
Language:
English
Publisher:
Wiley
Publication Date:
2008
detail.hit.zdb_id:
2209649-8
SSG:
15,3
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