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pro vyhledávání: '"David William End"'
Autor:
Ashis K. Saha, David William End
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:1713-1719
Solid-phase synthesis of imidazolyl-beta-amino acid derivatives is described. Several analogs demonstrated moderate inhibition of geranylgeranyl protein transferase type I (GGPT I).
Autor:
Patrick Rene Angibaud, Eddy Jean Edgard Freyne, Christophe Meyer, Jacky Van Dun, Gerda Smets, Marc Venet, Isabelle Noëlle Constance Pilatte, Laurence Mevellec, Virginie Sophie Poncelet, Bruno Roux, Geert Mannens, Ashis K. Saha, David William End, Wouters Walter Boudewijn Leopo, Xavier Bourdrez, Patricia Lezouret
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:4361-4364
Replacement of the 1-methylimidazol-5-yl moiety in the farnesyltransferase inhibitor ZARNESTRA series by a 4-methyl-1,2,4-triazol-3-yl group gave us compounds with similar structure-activity relationship profiles showing that this triazole is potenti
Autor:
Gerda Smets, Laurence Mevellec, Michel Janicot, Pieter Van Remoortere, Bruno Roux, Yannick Aimé Eddy Ligny, Isabelle Noëlle Constance Pilatte, Jacky Van Dun, Wouters Walter Boudewijn Leopo, Xavier Bourdrez, Patrick Rene Angibaud, Geert Mannens, Marc Venet, David William End, Philippe Muller, Christophe Meyer, Patricia Lezouret, Siegrid Damsch, Eddy Jean Edgard Freyne, Virginie Sophie Poncelet
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:4365-4369
A series of (4-chlorophenyl)-alpha-(1-methyl-1H-imidazol-5-yl)azoloquinolines and -quinazolines was prepared. These compounds displayed potent Farnesyl Protein Transferase inhibitory activity and tetrazolo[1,5-a]quinazolines are promising agents for
Publikováno v:
Current Topics in Medicinal Chemistry. 3:1095-1102
R115777 (R)-6-amino[(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl]-4-(3-chlorophenyl)-1-methyl-2(1H)-quinolinone is a potent and selective inhibitor of farnesyl protein transferase with significant antitumor effects in vivo subsequent to oral adm
Autor:
David William End
Publikováno v:
Investigational new drugs. 17(3)
The year 2000 will be a significant date for the field of Ras-related therapies since numerous agents will have Phase II clinical efficacy data maturing to provide proof of principle for this cancer treatment strategy. These data will also provide an
Publikováno v:
Journal of pharmacological and toxicological methods. 34(4)
A simple method was developed to detect the metabolism of [3H]-retinoic acid to polar products using intact tumor cells in culture. Unaltered [3H]-retinoic acid was separated from more polar metabolites using C18-bonded solid phase extraction cartrid