Document Report Card
Basic Information
ID: ALA1133972
Journal: Bioorg Med Chem Lett
Title: Solid-Phase synthesis of a library constructed of aromatic phosphate, long alkyl chains and tryptophane components, and identification of potent dipeptide telomerase inhibitors.
Authors: Sasaki S, Ehara T, Alam MR, Fujino Y, Harada N, Kimura J, Nakamura H, Maeda M.
Abstract: 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 IC(50) values of 0.3 microM. A hypothetical binding model for the new inhibitors has been proposed based on the structure-activity relationship.
CiteXplore: 11551754