TY - JOUR
T1 - Solid-phase synthesis of a library constructed of aromatic phosphate, long alkyl chains and tryptophane components, and identification of potent dipeptide telomerase inhibitors
AU - Sasaki, Shigeki
AU - Ehara, Takeru
AU - Alam, Md Rowshon
AU - Fujino, Yasuhiro
AU - Harada, Naozumi
AU - Kimura, Junko
AU - Nakamura, Hideo
AU - Maeda, Minoru
N1 - Copyright:
Copyright 2007 Elsevier B.V., All rights reserved.
PY - 2001/10/8
Y1 - 2001/10/8
N2 - Telomerase inhibitors are expected as a new candidate of therapeutic agents for cancer. Recently, we have found novel inhibitors based on the bisindole skeleton. In this study, solid-phase synthesis was applied to construct a library of inhibitors having aromatic phosphate, long alkyl chain and tryptophane components, from which a D,D-ditryptophane derivative has been identified as a new potent telomerase inhibitor with IC50 values of 0.3 μM. A hypothetical binding model for the new inhibitors has been proposed based on the structure-activity relationship.
AB - Telomerase inhibitors are expected as a new candidate of therapeutic agents for cancer. Recently, we have found novel inhibitors based on the bisindole skeleton. In this study, solid-phase synthesis was applied to construct a library of inhibitors having aromatic phosphate, long alkyl chain and tryptophane components, from which a D,D-ditryptophane derivative has been identified as a new potent telomerase inhibitor with IC50 values of 0.3 μM. A hypothetical binding model for the new inhibitors has been proposed based on the structure-activity relationship.
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U2 - 10.1016/S0960-894X(01)00507-8
DO - 10.1016/S0960-894X(01)00507-8
M3 - Article
C2 - 11551754
AN - SCOPUS:0035829149
SN - 0960-894X
VL - 11
SP - 2581
EP - 2584
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 19
ER -
