Synthesis of novel, peptidic kinase inhibitors with cytostatic/cytotoxic activity

Wiktor Szymanski, Magdalena Zwolinska, Szymon Klossowski, Izabela Mlynarczuk-Bialy, Lukasz Bialy, Tadeusz Issat, Jacek Malejczyk, Ryszard Ostaszewski*

*Bijbehorende auteur voor dit werk

OnderzoeksoutputAcademicpeer review

13 Citaten (Scopus)


The utility of a novel, chemoenzymatic procedure for the stereocontrolled synthesis of small peptides is presented in the preparation and structure optimisation of dipeptides with cytostatic/cytotoxic activity. The method uses Passerini multicomponent reaction for the preparation of racemic scaffold which is then enantioselectively hydrolysed by hydrolytic enzymes. Products of these transformations are further functionalised towards title compounds. Both activity and selectivity towards tumor cells is optimised. Final compound is shown to be an inhibitor of the protein kinase signaling pathway. (C) 2014 Elsevier Ltd. All rights reserved.

Originele taal-2English
Pagina's (van-tot)1773-1781
Aantal pagina's9
TijdschriftBioorganic & Medicinal Chemistry
Nummer van het tijdschrift5
StatusPublished - 1-mrt-2014

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