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Design and Synthesis of an Optimized Positional Scanning Library of Peptoids: Identification of Novel Multidrug Resistance Reversal Agents by Isabel Masip; Nuria Cortés; Maria-José Abad; Marisa Guardiola; Enrique Pérez-Payá; José Ferragut; Antonio Ferrer-Montiel; Angel Messeguer is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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Herein is reported the optimized solid-phase synthesis of a library of 5,120 trimeric N-alkylglycines (peptoids) using the positional scanning format and the submonomer strategy. Diversity at the N-terminal position was generated from 20 commercially available primary amines, whereas 16 primary amines were employed for the middle and C-terminal positions of the trimers. Formation of undesirable side-products observed in a previous library synthesis (Humet, M. et al. J. Comb. Chem. 2003, 5, 597-605) was averted by restricting the use of primary amines functionalized with tertiary amino groups to the third amination step. Screening of the new library for the identification of chemosensitizers yielded two peptoids, compounds 1 and 2, with potent in vitro activity as multidrug resistance (MDR) reversal agents. The structures of the lead peptoids are consistent with a pharmacophore model generated from the interaction of various known inhibitors with the MDR-implicated transmembrane glycoprotein P-gp.

Who reads Design and Synthesis of an Optimized Positional Scanning Library of Peptoids: Identification of Novel Multidrug Resistance Reversal Agents?

Author

Isabel Masip; Nuria Cortés; Maria-José Abad; Marisa Guardiola; Enrique Pérez-Payá; José Ferragut; Antonio Ferrer-Montiel; Angel Messeguer

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)

Published

2005

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)