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Your search keyword '"Scheeren, H.W."' showing total 27 results
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27 results on '"Scheeren, H.W."'

4. High-pressure-mediated extension of the privileged steroid scaffold

Author

Blanco-Ania, D., Aben, R.W.M., Berkom, L.W.A. van, Scheeren, H.W., and Rutjes, F.P.J.T.

Subjects
Synthetic Organic Chemistry, Physical Organic Chemistry
Abstract

Contains fulltext : 123205.pdf (Author’s version postprint ) (Open Access) Contains fulltext : 123205.pdf (Publisher’s version ) (Open Access)

Published
2013

10. Design, synthesis, and biological evaluation of a dual tumor-specific motive containing integrin-targeted plasmin-cleavable doxorubicin prodrug

Author

de Groot, FMH, Broxterman, HJ, Adams, HPHM, van Vliet, A, Tesser, GI, Elderkamp, YW, Leegte - Schraa, Astrid, Kok, RJ, Molema, G, Pinedo, HM, Scheeren, H.W., Nanomedicine & Drug Targeting, Groningen Kidney Center (GKC), and Critical care, Anesthesiology, Peri-operative and Emergency medicine (CAPE)

Subjects
SELECTIVE ACTIVATION, CELLS, VASCULATURE, PROTEASE PLASMIN, ANTICANCER DRUGS, PEPTIDES, SOLID-PHASE SYNTHESIS, CHEMOTHERAPY, CANCER, IN-VIVO
Abstract

The design, synthesis, and initial biological evaluation of a doxorubicin prodrug that contains a dual tumor specific moiety, which allows enhanced tumor recognition potential, is reported. Both a tumor-specific recognition site and a tumor selective enzymatic activation sequence are incorporated in the prodrug. The first tumor-specific sequence is the bicyclic CDCRGDCFC (RGD-4C) peptide that selectively binds alpha(v)beta(3) and alpha(v)beta(5) integrins. These integrins are highly overexpressed on invading tumor endothelial cells. The second tumor-specific sequence is a D-Ala-Phe-Lys tripeptide that is selectively recognized by the tumor-associated protease plasmin, which is involved in tumor invasion and metastasis. An aminocaproyl residue was incorporated as a spacer between the two peptide sequences, whereas a self-eliminating 4-aminobenzyl alcohol spacer was inserted between the plasmin substrate and doxorubicin. Although the prodrug showed a decreased binding affinity as compared with the unconjugated reference peptide, it was still a potent ligand for alpha(v)beta(3) and alpha(v)beta(5) integrin receptors. The synthesized construct also possessed plasmin substrate properties as demonstrated by doxorubicin release from 1 upon incubation with plasmin. The release of doxorubicin from 1 was not complete, possibly related to low prodrug solubility. In vitro prodrug 1 showed plasmin-dependent cytotoxicity for endothelial cells and HT1080 fibrosarcoma cells. On the basis of these in vitro results, derivatives of 1 with improved water solubility are considered good candidates for additional development and in vivo evaluation of this dual targeting concept.

Published
2002

21. Synthesis of spirohydantoins and spiro-2,5-diketopiperazines via resin-bound cyclic alpha,alpha-disubstituted alpha-amino esters

Author

Kuster, G.J.T., Kalmoua, M., Loevezijn, A. van, Sliedregt, L.A.J.M., Steen, B.J. van, Kruse, C.G., Rutjes, F.P.J.T., Scheeren, H.W., Kuster, G.J.T., Kalmoua, M., Loevezijn, A. van, Sliedregt, L.A.J.M., Steen, B.J. van, Kruse, C.G., Rutjes, F.P.J.T., and Scheeren, H.W.

Abstract

Contains fulltext : 33042.pdf (publisher's version ) (Closed access)

Published
2005

26. Semisynthesis of some 7-deoxypaclitaxel analogs from taxine B

Author

Wiegerinck, P.H.G., Fluks, L., Hammink, J.B., Mulders, S.J.E., Groot, F.M.H. de, Rozendaal, H.L.M. van, Scheeren, H.W., Wiegerinck, P.H.G., Fluks, L., Hammink, J.B., Mulders, S.J.E., Groot, F.M.H. de, Rozendaal, H.L.M. van, and Scheeren, H.W.

Abstract

Contains fulltext : 28838___.PDF (publisher's version ) (Open Access)

Published
1996

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