Citation
Xb. Ding et al., Structure-activity relationships of side-chain modified didemnins, BIOORG MED, 11(2), 2001, pp. 231-234
Citations number
24
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X
→ ACNP
Volume
11
Issue
2
Year of publication
2001
Pages
231 - 234
Database
ISI
SICI code
0960-894X(20010122)11:2<231:SROSMD>2.0.ZU;2-C
Abstract
The synthesis and antitumor activity of a novel didemnin B analogue contain
ing a Psi [CH2NH] amide bond surrogate between N-Me-D-Leu(7) and pro(8) are
reported. The analogue shows activity (GI(50) = 4 nM) comparable to that o
f didemnin B (GI(50) = 13 nM) in the NCI-60 tumor cell screen. This result,
along with new data from previously reported synthetic didemnin analogues,
is discussed within the context of the side-chain SAR for didemnins. (C) 2
001 Elsevier Science Ltd. All rights reserved.