Substituent effects within the DNA binding subunit of CBI analogues of theduocarmycins and CC-1065

Authors
Boger, DL Stauffer, F Hedrick, MP
Citation
Dl. Boger et al., Substituent effects within the DNA binding subunit of CBI analogues of theduocarmycins and CC-1065, BIOORG MED, 11(15), 2001, pp. 2021-2024
Citations number
34
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
15
Year of publication
2001
Pages
2021 - 2024
Database
ISI
SICI code
0960-894X(20010806)11:15<2021:SEWTDB>2.0.ZU;2-7
Abstract
A series of CBI analogues of the duocarmycins and CC-1065 exploring substit uent effects within the first indole DNA binding subunit are detailed. Subs titution at the indole C5 position led to cytotoxic potency enhancements th at are greater than or equal to 1000-fold, providing simplified analogues c ontaining a single DNA binding subunit that are more potent (IC50 = 2-3 pM) than CBI-TMI, duocarmycin SA, or CC-1065. (C) 2001 Elsevier Science Ltd. A ll rights reserved.