Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
Non-amide-based combinatorial libraries derived from N-Boc-iminodiacetic acid: Solution-phase synthesis of piperazinone libraries with activity against LEF-1/beta-catenin-mediated transcription
Autore:
Boger, DL; Goldberg, J; Satoh, S; Ambroise, Y; Cohen, SB; Vogt, PK;
Indirizzi:
Scripps Clin & Res Inst, Dept Chem, La Jolla, CA 92037 USA Scripps Clin & Res Inst La Jolla CA USA 92037 hem, La Jolla, CA 92037 USA Scripps Clin & Res Inst, Skaggs Inst Chem Biol, La Jolla, CA 92037 USA Scripps Clin & Res Inst La Jolla CA USA 92037 iol, La Jolla, CA 92037 USA Scripps Clin & Res Inst, Dept Mol & Expt Med, La Jolla, CA 92037 USA Scripps Clin & Res Inst La Jolla CA USA 92037 Med, La Jolla, CA 92037 USA
Titolo Testata:
HELVETICA CHIMICA ACTA
fascicolo: 8, volume: 83, anno: 2000,
pagine: 1825 - 1845
SICI:
0018-019X(2000)83:8<1825:NCLDFN>2.0.ZU;2-2
Fonte:
ISI
Lingua:
ENG
Soggetto:
SMALL ORGANIC-MOLECULES; PROTEIN-PROTEIN INTERACTIONS; OLEFIN METATHESIS REACTION; CHIRAL PIPERAZIN-2-ONE; EFFICIENT SYNTHESIS; CHEMICAL LIBRARIES; GENERAL-METHOD; SOLID SUPPORT; DNA-BINDING; 2-OXOPIPERAZINES;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Physical, Chemical & Earth Sciences
Citazioni:
49
Recensione:
Indirizzi per estratti:
Indirizzo: Boger, DL Scripps Clin & Res Inst, Dept Chem, 10550 N Torrey Pines Rd, La Jolla, CA 92037 USA Scripps Clin & Res Inst 10550 N Torrey Pines Rd La Jolla CA USA 92037
Citazione:
D.L. Boger et al., "Non-amide-based combinatorial libraries derived from N-Boc-iminodiacetic acid: Solution-phase synthesis of piperazinone libraries with activity against LEF-1/beta-catenin-mediated transcription", HELV CHIM A, 83(8), 2000, pp. 1825-1845

Abstract

The development of a solution-phase approach to the rapid, parallel synthesis of highly functionalized piperazinones in only four steps starting fromN-Boc-iminodiacetic acid is detailed. The efforts represent the extension of the solution-phase synthesis of combinatorial libraries from N-Boc-iminodiacetic acid to nonamide-based libraries where simple liquid-liquid extractions are employed to purify all reaction products. This methodology was applied to the synthesis of a diverse 150-member library with substituents inthree positions of the piperazinone core. Screening results from a luciferase reporter assay indicate that a number of library members are novel repressors of LEF-1/beta-catenin-mediated transcription, and may be effective agents against colorectal tumors. Two secondary libraries (100 members each)designed from these lead structures were synthesized and screened, providing additional active agents and insight into key structure-activity relationships in the series. These compounds represent only the second class of small molecules which repress transcription of reporter genes containing LEF-1 responsive elements, and the first group not based on DNA minor-groove-binding agents.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 07/07/20 alle ore 22:14:40