1 to 10 of 19 literature results

• 4-Oxo-beta-lactams (azetidine-2,4-diones) are potent and selective inhibitors of human leukocyte elastase.

  Human leukocyte elastase (HLE) is a serine protease stored in and secreted from neutrophils that plays a determinant role in the pathogenesis of sever…

  Authors: Jalmira Mulchande, Rudi Oliveira, Marta Carrasco, Luís Gouveia, Rita C Guedes, Jim Iley, Rui Moreira

  Source: Journal of medicinal chemistry. 2010 Jan 14

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• Azetidine-2,4-diones (4-oxo-beta-lactams) as scaffolds for designing elastase inhibitors.

  A new class of inhibitors 4-oxo-beta-lactams (azetidine-2,4-diones), containing the required structural elements for molecular recognition, inhibit po…

  Authors: Jalmira Mulchande, Rita C Guedes, Wing-Yin Tsang, Michael I Page, Rui Moreira, Jim Iley

  Source: Journal of medicinal chemistry. 2008 Mar 27

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• Reaction of naphthoquinones with substituted nitromethanes. Facile synthesis and antifungal activity of naphtho[2,3-d]isoxazole-4,9-diones.

  We report here a simple entry into naphtho[2,3-d]isoxazole-4,9-dione system containing a EWG in position 3 using the readily available 2,3-dichloro-1,…

  Authors: Maria M M Santos, Natália Faria, Jim Iley, Simon J Coles, Michael B Hursthouse, M Luz Martins, Rui Moreira

  Source: Bioorganic & medicinal chemistry letters. 2010 Jan 1

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• Towards an efficient prodrug of the alkylating metabolite monomethyltriazene: synthesis and stability of N-acylamino acid derivatives of triazenes.

  A series of 3-[alpha-(acylamino)acyl]-1-aryl-3-methyltriazenes 6a-l, potential cytotoxic triazene prodrugs, were synthesised by coupling 1-aryl-3-meth…

  Authors: Maria de Jesus Perry, Emília Carvalho, Eduarda Rosa, Jim Iley

  Source: European journal of medicinal chemistry. 2009 Mar

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• Structure-activity studies of the binding of the flavonoid scaffold to DNA.

  BACKGROUND: Flavonoids have been shown to have a wide variety of biological activities and proven to be good scaffolds for the design of DNA-binding a…

  Authors: Patricia A Ragazzon, Jim Iley, Sotiris Missailidis

  Source: Anticancer research. 2009 Jun

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• The characterisation of flavone-DNA isoform interactions as a basis for anticancer drug development.

  BACKGROUND: The interactions of small molecules with nucleic acids are of considerable interest for the design of novel anticancer compounds. The phys…

  Authors: Patricia A Ragazzon, Tracey Bradshaw, Charlie Matthews, Jim Iley, Sotiris Missailidis

  Source: Anticancer research. 2009 Jun

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• Design, synthesis, and enzymatic evaluation of N1-acyloxyalkyl- and N1-oxazolidin-2,4-dion-5-yl-substituted beta-lactams as novel inhibitors of human leukocyte elastase.

  Human leukocyte elastase (HLE) is a serine protease that very efficiently degrades various tissue matrix proteins such as elastin. The imbalance betwe…

  Authors: Rui Moreira, Ana Bela Santana, Jim Iley, João Neres, Kenneth T Douglas, Peter N Horton, Michael B Hursthouse

  Source: Journal of medicinal chemistry. 2005 Jul 28

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• Dopamine- and tyramine-based derivatives of triazenes: activation by tyrosinase and implications for prodrug design.

  A range of triazene derivatives were synthesized and investigated as prodrug candidates for melanocyte-directed enzyme prodrug therapy (MDEPT). The pr…

  Authors: M Jesus Perry, Eduarda Mendes, Ana Luísa Simplício, Ana Coelho, Ricardo V Soares, Jim Iley, Rui Moreira, Ana Paula Francisco

  Source: European journal of medicinal chemistry. 2009 Aug

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• The Bsmoc group as a novel scaffold for the design of irreversible inhibitors of cysteine proteases.

  Carbamate and ester derivatives of the 1,1-dioxobenzo[b]thiophen-2-ylmethyloxycarbonyl (Bsmoc) scaffold react readily with thiols via a Michael additi…

  Authors: Jim Iley, Rui Moreira, Luísa Martins, Rita C Guedes, Cláudio M Soares

  Source: Bioorganic & medicinal chemistry letters. 2006 May 15

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• The 1,4-naphthoquinone scaffold in the design of cysteine protease inhibitors.

  A series of 1,4-naphthoquinone derivatives diversely substituted at C-2, C-3, C-5 and C-8, prepared by reaction of amines, amino acids and alcohols wi…

  Authors: Cláudia Valente, Rui Moreira, Rita C Guedes, Jim Iley, Mohammed Jaffar, Kenneth T Douglas

  Source: Bioorganic & medicinal chemistry. 2007 Aug 1

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