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  • Open Daily: 10am - 10pm
    Alley-side Pickup: 10am - 7pm

    3038 Hennepin Ave Minneapolis, MN
    612-822-4611

Open Daily: 10am - 10pm | Alley-side Pickup: 10am - 7pm
3038 Hennepin Ave Minneapolis, MN
612-822-4611
Design, Synthesis and Evaluation of Highly Functionalized Peptoids as Antitumor Peptidomimetics

Design, Synthesis and Evaluation of Highly Functionalized Peptoids as Antitumor Peptidomimetics

Cardenal, Carmen

Paperback

Series: Beiträge Zur Organischen Synthese, Book 47

Chemistry

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ISBN10: 383253721X
ISBN13: 9783832537210
Publisher: Logos Verlag Berlin
Published: Jun 20 2014
Pages: 170
Weight: 0.55
Height: 0.48 Width: 5.68 Depth: 8.04
Language: English
Peptides perform a wide variety of essential functions in living organisms with great specificity and precision. However, their therapeutic use is limited, due to their fast degradation by proteases in vivo and consequent poor oral bioavailability. Thanks to their proteolytic resistance and easily accessible and derivatizable synthesis on solid supports, peptoids (N-substituted glycine oligomers) have emerged as promising peptidomimetics for biological and medical applications. In this work peptoid analogs of two short amino acid sequences with antitumor activity (one derived from the CD44-v6 coreceptor and one from the BAG-1L protein), have been designed and synthesized. Comparison of the biological activity of the peptides and the different peptoid analogs led to the establishment of structure-activity relationships and the identification of a lead compound showing high potential for cancer therapy. In addition, a method for the synthesis of amide-containing submonomers as free bases and their incorporation into peptoid oligomers is described. Different-length homo-oligomers of alpha-chiral amide residues were successfully synthesized for structural investigations.

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