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1.	Hadimani, MB, et al. (author) Synthesis, in vitro, and in vivo evaluation of phosphate ester derivatives of combretastatin A-4 2003 In: Bioorganic & Medicinal Chemistry Letters. - 0960-894X. ; 13:9, s. 1505-1508 Journal article (peer-reviewed)abstract Combretastatin A-4 disodiumphosphate (CA4P), a prodrug formulation of the natural product combretastatin A-4 (CA4), is currently in clinical investigation for the treatment of cancer. In vivo, CA4P is rapidly enzymatically converted to CA4, a potent inhibitor of tubulin polymerization (IC50 = 1-2 muM), and rapidly causes bloodflow shutdown in tumor tissues. A variety of alkyl and aryl di- and triesters of CA4P have been synthesized and evaluated as potential CA4 prodrugs and/or stable CAV analogues. (C) 2003 Elsevier Science Ltd. All rights reserved.
2.	Berglund, P., et al. (author) Altering the specificity of subtilisin B. lentus by combining site-directed mutagenesis and chemical modification 1996 In: Bioorganic & Medicinal Chemistry Letters. - 0960-894X .- 1464-3405. ; 6:21, s. 2507-2512 Journal article (peer-reviewed)abstract The thiol side chain of the M222C mutant of the subtilisin from Bacillus lentus (SBL) has been chemically modified by methyl-, aminoethyl-, and sulfonatoethylthiosulfonate reagents. Introduction of charged residues into the active site of the enzyme reduced the catalytic efficiency with Suc-AAPF-pNA as the substrate, but resulted in better binding of sterically demanding boronic acid inhibitors.
3.	Carini, DJ, et al. (author) Identification of selective inhibitors of cyclin dependent kinase 4 2001 In: Bioorganic & medicinal chemistry letters. - 0960-894X. ; 11:16, s. 2209-2211 Journal article (peer-reviewed)
4.	Hernandez, AI, et al. (author) Improving the selectivity of acyclic nucleoside analogues as inhibitors of human mitochondrial thymidine kinase: replacement of a triphenylmethoxy moiety with substituted amines and carboxamides 2003 In: Bioorganic & medicinal chemistry letters. - : Elsevier BV. - 0960-894X. ; 13:18, s. 3027-3030 Journal article (peer-reviewed)
5.	Johansson, Anja, et al. (author) Inhibition of hepatitis C virus NS3 protease activity by product-based peptides is dependent on helicase domain 2001 In: Bioorganic & Medicinal Chemistry Letters. - 0960-894X .- 1464-3405. ; 11:2, s. 203-206 Journal article (peer-reviewed)
6.	Jönsson, Christina, et al. (author) Immobilized oxazoline-containing ligands in asymmetric catalysis - A review 2002 In: Bioorganic & Medicinal Chemistry Letters. - 0960-894X .- 1464-3405. ; 12:14, s. 1857-1861 Research review (peer-reviewed)abstract Metal complexes of chiral oxazoline derivatives immobilized on soluble as well as insoluble supports serve as versatile asymmetric catalysts in a variety of applications. In a few cases recovery and reuse of the chiral ligands have been achieved.
7.	Manfredini, S, et al. (author) Design, synthesis and enzymatic activity of highly selective human mitochondrial thymidine kinase inhibitors 2001 In: Bioorganic & medicinal chemistry letters. - 0960-894X. ; 11:10, s. 1329-1332 Journal article (peer-reviewed)
8.	Sandell, J, et al. (author) Synthesis, radiolabeling and preliminary biological evaluation of radiolabeled 5-methyl-6-nitroquipazine, a potential radioligand for the serotonin transporter 2002 In: Bioorganic & medicinal chemistry letters. - 0960-894X. ; 12:24, s. 3611-3613 Journal article (peer-reviewed)
9.	Aili, Ulrika, et al. (author) Antiproliferative effects of peracetylated naphthoxylosides. 2009 In: Bioorganic & Medicinal Chemistry Letters. - : Elsevier BV. - 0960-894X. ; 19, s. 1763-1766 Journal article (peer-reviewed)abstract The antiproliferative activity, and the capability of priming of glycosaminoglycan chains, of two series of peracetylated mono- and bis-xylosylated dihydroxynaphthalenes have been investigated for normal HFL-1 cells, as well as transformed T24 cells, and compared to the unprotected analogs. Our data show increased antiproliferative activity upon peracetylation, but a loss of selectivity towards T24 cells.
10.	Andaloussi, Mounir, et al. (author) Substitution of the phosphonic acid and hydroxamic acid functionalities of the DXR inhibitor FR900098 : An attempt to improve the activity against Mycobacterium tuberculosis 2011 In: Bioorganic & Medicinal Chemistry Letters. - : Elsevier BV. - 0960-894X .- 1464-3405. ; 21:18, s. 5403-5407 Journal article (peer-reviewed)abstract Two series of FR900098/fosmidomycin analogs were synthesized and evaluated for MtDXR inhibition and Mycobacterium tuberculosis whole-cell activity. The design rationale of these compounds involved the exchange of either the phosphonic acid or the hydroxamic acid part for alternative acidic and metal-coordinating functionalities. The best inhibitors provided IC(50) values in the micromolar range, with a best value of 41 mu M.

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Type of publication: journal article (80); research review (1)

Type of content: peer-reviewed (81)

Author/Editor: Larhed, Mats (7); Halldin, C (5); Leffler, Hakon (4); Hallberg, Anders (4); Arvidsson, Per I. (3); Odell, Luke R (3); show more...; Nilsson, Ulf (3); Mani, Katrin (3); Ellervik, Ulf (3); Samuelsson, Bertil (3); Nilsson, Magnus (2); Helleday, Thomas (2); Nilsson, Peter (2); Sterner, Olov (2); Jacobsson, Mårten (2); Schneider, G (2); Vrang, Lotta (2); Rosenquist, Åsa (2); Karlén, Anders (2); Varnas, K (2); Agback, Tatiana (2); Loseva, Olga (2); Schnell, R (2); Karlsson, A. (2); Nilsson, Jakob (2); Johnsson, Richard (2); Nag, S (2); Gulyas, B (2); Govender, Thavendran (2); Kruger, Hendrik G. (2); Schuler, H. (2); Schaal, Wesley (2); Boesen, Thomas (2); Maguire, Glenn E. M. (2); Schou, M (2); Wallinder, Charlotta (2); Claesson, Hans-Erik (2); Nielsen, Mogens (2); Pike, VW (2); Sandell, J (2); Arakawa, R (2); Balzarini, J (2); Hallberg, Mathias, 1 ... (2); Martens, Ulf (2); Häggblad, Maria (2); Lundgren, Bo (2); Liljefors, Tommy (2); Scobie, Martin (2); Jemth, Ann-Sofie (2); Llona-Minguez, Sabin (2); show less...

University: Karolinska Institutet (29); Uppsala University (25); Lund University (12); Stockholm University (8); Umeå University (7); Royal Institute of Technology (7); show more...; Linköping University (2); University of Gothenburg (1); Mid Sweden University (1); RISE (1); Swedish University of Agricultural Sciences (1); show less...

Language: English (81)

Research subject (UKÄ/SCB): Medical and Health Sciences (34); Natural sciences (25); Engineering and Technology (1); Agricultural Sciences (1)

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