M Amelia Santos

Summary

Country: Portugal

Publications

  1. ncbi Design, synthesis and molecular modeling study of iminodiacetyl monohydroxamic acid derivatives as MMP inhibitors
    M Amelia Santos
    Centro de Quimica Estrutural, Instituto Superior Tecnico, Rua Rovisco Pais 1, 1049 001 Lisboa, Portugal
    Bioorg Med Chem 14:7539-50. 2006
  2. ncbi Iminodiacetyl-hydroxamate derivatives as metalloproteinase inhibitors: equilibrium complexation studies with Cu(II), Zn(II) and Ni(II)
    Silvia Chaves
    Centro de Quimica Estrutural, Complexo I, Instituto Superior Tecnico, Av Rovisco Pais, 1049 001, Lisboa, Portugal
    J Inorg Biochem 97:345-53. 2003
  3. ncbi N-Arylamine derivatives of 3-hydroxy-4-pyridinones: solution studies and bioevaluation in view of Al-detoxification roles
    M Amelia Santos
    Centro de Quimica Estrutural, Complexo I, Instituto Superior Tecnico, Av Rovisco Pais, 1049 001 Lisboa, Portugal
    Anal Bioanal Chem 381:413-9. 2005
  4. ncbi Bis(3-hydroxy-4-pyridinone)-EDTA derivative as a potential therapeutic Al-chelating agent. Synthesis, solution studies and biological assays
    M Amelia Santos
    Centro de Quimica Estrutural, Complexo I, Instituto Superior Tecnico, Av Rovisco Pais, 1, 1049 001 Lisboa, Portugal
    J Inorg Biochem 99:1845-52. 2005
  5. ncbi Bifunctional 3-hydroxy-4-pyridinone derivatives as potential pharmaceuticals: synthesis, complexation with Fe(III), Al(III) and Ga(III) and in vivo evaluation with 67Ga
    M Amelia Santos
    Centro de Quimica Estrutural, Complexo I, Instituto Superior Tecnico, 1049 001 Lisboa, Portugal
    J Biol Inorg Chem 10:564-80. 2005
  6. ncbi Methotrexate gamma-hydroxamate derivatives as potential dual target antitumor drugs
    M Amelia Santos
    Centro de Quimica Estrutural, Instituto Superior Tecnico, 1049 001 Lisboa, Portugal
    Bioorg Med Chem 15:1266-74. 2007
  7. ncbi Carbonic anhydrase inhibitors: inhibition of cytosolic/tumor-associated isoforms I, II, and IX with iminodiacetic carboxylates/hydroxamates also incorporating benzenesulfonamide moieties
    M Amelia Santos
    Centro de Quimica Estrutural, Instituto Superior Tecnico, Rua Rovisco Pais 1, 1049 001 Lisbon, Portugal
    Bioorg Med Chem Lett 17:1538-43. 2007
  8. ncbi A new approach for potential combined chelation therapy using mono- and bis-hydroxypyridinones
    M Amelia Santos
    Centro de Quimica Estrutural, Instituto Superior Tecnico, Lisboa, Portugal
    Hemoglobin 32:147-56. 2008
  9. ncbi Novel folate-hydroxamate based antimetabolites: synthesis and biological evaluation
    Marta P Carrasco
    Centro de Quimica Estrutural, Instituto Superior Tecnico, 1049 001 Lisboa, Portugal
    Med Chem 7:265-74. 2011
  10. ncbi Novel 1-hydroxypiperazine-2,6-diones as new leads in the inhibition of metalloproteinases
    Sérgio M Marques
    Centro de Química Estrutural, Instituto Superior Tecnico, Av Rovisco Pais 1, 1049 001 Lisboa, Portugal
    J Med Chem 54:8289-98. 2011

Collaborators

  • Armando Rossello
  • Tiziano Tuccinardi
  • Claudiu T Supuran
  • Eva A Enyedy
  • Hiromu Sakurai
  • Etelka Farkas
  • Yutaka Yoshikawa
  • Catarina R Oliveira
  • Sérgio M Marques
  • Silvia Chaves
  • Adriano Martinelli
  • Elisa Nuti
  • Jaroslav Sebestik
  • Salvatore Santamaria
  • Marta P Carrasco
  • Raquel Grazina
  • Sergey A Krupenko
  • Natalia I Krupenko
  • M Alexandra Esteves
  • Lurdes Gano
  • M Luísa M Serralheiro
  • Sandra M Cardoso
  • Daniela M Arduino
  • Ana C Mendonça
  • Pedro L Falé
  • Susana Santos
  • Vânia André
  • André F Martins
  • Carlos F G C Geraldes
  • Ana C Santos
  • M Isabel Prata
  • Osvaldo Ortet
  • Ratomir Jelic
  • Catarina Mendonça
  • Anabela Capelo
  • André M F Matos
  • Marta Carrasco
  • Andreia Nunes
  • Paul I Dron
  • Florina A Danalache
  • Diana Sacoto
  • Sergio Marques

Detail Information

Publications20

  1. ncbi Design, synthesis and molecular modeling study of iminodiacetyl monohydroxamic acid derivatives as MMP inhibitors
    M Amelia Santos
    Centro de Quimica Estrutural, Instituto Superior Tecnico, Rua Rovisco Pais 1, 1049 001 Lisboa, Portugal
    Bioorg Med Chem 14:7539-50. 2006
    ..The sulfonamide based IDA derivatives studied (compounds B1-B3) showed to be potent (nM range) against deep S1' pocket MMPs enzymes (i.e., MMP-2)...
  2. ncbi Iminodiacetyl-hydroxamate derivatives as metalloproteinase inhibitors: equilibrium complexation studies with Cu(II), Zn(II) and Ni(II)
    Silvia Chaves
    Centro de Quimica Estrutural, Complexo I, Instituto Superior Tecnico, Av Rovisco Pais, 1049 001, Lisboa, Portugal
    J Inorg Biochem 97:345-53. 2003
    ..Moreover, at higher pH, H(2)L(1) is able to form a pentanuclear tetrameric copper complex with an interesting 12-metallacrown-4 structure...
  3. ncbi N-Arylamine derivatives of 3-hydroxy-4-pyridinones: solution studies and bioevaluation in view of Al-detoxification roles
    M Amelia Santos
    Centro de Quimica Estrutural, Complexo I, Instituto Superior Tecnico, Av Rovisco Pais, 1049 001 Lisboa, Portugal
    Anal Bioanal Chem 381:413-9. 2005
    ....
  4. ncbi Bis(3-hydroxy-4-pyridinone)-EDTA derivative as a potential therapeutic Al-chelating agent. Synthesis, solution studies and biological assays
    M Amelia Santos
    Centro de Quimica Estrutural, Complexo I, Instituto Superior Tecnico, Av Rovisco Pais, 1, 1049 001 Lisboa, Portugal
    J Inorg Biochem 99:1845-52. 2005
    ..Biodistribution studies, performed with 67Ga-overload mice, showed rapid clearance of the radiotracer from the body, thus indicating that the new ligand should be a quite effective agent for the in vivo aluminium removal...
  5. ncbi Bifunctional 3-hydroxy-4-pyridinone derivatives as potential pharmaceuticals: synthesis, complexation with Fe(III), Al(III) and Ga(III) and in vivo evaluation with 67Ga
    M Amelia Santos
    Centro de Quimica Estrutural, Complexo I, Instituto Superior Tecnico, 1049 001 Lisboa, Portugal
    J Biol Inorg Chem 10:564-80. 2005
    ..Concerning the (67)Ga complexes, the benzyl-propylamine (H(2)L(3)) shows considerable bone retention, thus suggesting its potential application as imaging agent...
  6. ncbi Methotrexate gamma-hydroxamate derivatives as potential dual target antitumor drugs
    M Amelia Santos
    Centro de Quimica Estrutural, Instituto Superior Tecnico, 1049 001 Lisboa, Portugal
    Bioorg Med Chem 15:1266-74. 2007
    ..Therefore, based on the present results, these bi-functional drugs may be good candidates to target specific tumors in animal models due to potential combined effects on two pathways crucial for tumor development...
  7. ncbi Carbonic anhydrase inhibitors: inhibition of cytosolic/tumor-associated isoforms I, II, and IX with iminodiacetic carboxylates/hydroxamates also incorporating benzenesulfonamide moieties
    M Amelia Santos
    Centro de Quimica Estrutural, Instituto Superior Tecnico, Rua Rovisco Pais 1, 1049 001 Lisbon, Portugal
    Bioorg Med Chem Lett 17:1538-43. 2007
    ....
  8. ncbi A new approach for potential combined chelation therapy using mono- and bis-hydroxypyridinones
    M Amelia Santos
    Centro de Quimica Estrutural, Instituto Superior Tecnico, Lisboa, Portugal
    Hemoglobin 32:147-56. 2008
    ..This may be rationalized by adjuvant and eventual synergistic effects, due to complementary accessibility of each chelator to different cellular compartments...
  9. ncbi Novel folate-hydroxamate based antimetabolites: synthesis and biological evaluation
    Marta P Carrasco
    Centro de Quimica Estrutural, Instituto Superior Tecnico, 1049 001 Lisboa, Portugal
    Med Chem 7:265-74. 2011
    ..The MTX-based compound could be of interest for testing against metastasizing tumors in an animal model. The studied derivatives represent promising molecular templates for further development of dual activity anti-cancer drugs...
  10. ncbi Novel 1-hydroxypiperazine-2,6-diones as new leads in the inhibition of metalloproteinases
    Sérgio M Marques
    Centro de Química Estrutural, Instituto Superior Tecnico, Av Rovisco Pais 1, 1049 001 Lisboa, Portugal
    J Med Chem 54:8289-98. 2011
    ..The final structure obtained will allow straightforward drug design approaches in view of further optimization and development of new MMP inhibitors bearing the HPD moiety...
  11. ncbi New tris(hydroxypyridinones) as iron and aluminium sequestering agents: synthesis, complexation and in vivo studies
    Silvia Chaves
    Centro de Quimica Estrutural, Instituto Superior Tecnico, Av Rovisco Pais 1, 1049 001 Lisboa, Portugal
    Chemistry 16:10535-45. 2010
    ....
  12. ncbi N-Carboxyalkyl derivatives of 3-hydroxy-4-pyridinones: synthesis, complexation with Fe(III), Al(III) and Ga(III) and in vivo evaluation
    M Amelia Santos
    Centro de Quimica Estrutural, Complexo I, Instituto Superior Tecnico, Av Rovisco Pais, Lisbon, Portugal
    J Inorg Biochem 92:43-54. 2002
    ..All the ligands were found to enhance the excretion of the gallium. Noteworthy is the observed Ga bone fixation, mostly with the ethyl derivative, thus suggesting the potential use of the complex as a bone seeking agent...
  13. ncbi Dual inhibitors of matrix metalloproteinases and carbonic anhydrases: iminodiacetyl-based hydroxamate-benzenesulfonamide conjugates
    Sérgio M Marques
    Centro de Quimica Estrutural, Instituto Superior Tecnico, Av Rovisco Pais 1, 1049 001 Lisboa, Portugal
    J Med Chem 51:7968-79. 2008
    ..Furthermore, a docking study for MMPs was reported for the most promising compound in order to investigate its binding interactions with the different MMPs...
  14. ncbi Pteridine-sulfonamide conjugates as dual inhibitors of carbonic anhydrases and dihydrofolate reductase with potential antitumor activity
    Sérgio M Marques
    Instituto Superior Tecnico, Centro de Quimica Estrutural, Av Rovisco Pais 1, 1049 001 Lisboa, Portugal
    Bioorg Med Chem 18:5081-9. 2010
    ..Nevertheless, this fact points out the need of improving the cell intake properties of these new compounds, since the general inhibitory profiles revealed their potential as anticancer agents...
  15. ncbi New hydroxypyrimidinone-containing sulfonamides as carbonic anhydrase inhibitors also acting as MMP inhibitors
    M Alexandra Esteves
    LNEG, Unidade de Pilhas de Combustível e Hidrogénio, Estrada do Paco do Lumiar, Lisboa, Portugal
    Bioorg Med Chem Lett 20:3623-7. 2010
    ....
  16. ncbi Combined chelation based on glycosyl-mono- and bis-hydroxypyridinones for aluminium mobilization: solution and biodistribution studies
    Silvia Chaves
    Centro de Quimica Estrutural, Instituto Superior Tecnico, 1049 001 Lisboa, Portugal
    J Inorg Biochem 103:1521-9. 2009
    ..This may be rationalized by coadjuvation and eventual synergistic effects, due to complementary accessibility of the chelators to different cellular compartments...
  17. ncbi New hydroxypyridinone-functionalized sepharoses as sorbing agents for hard metal ions
    Raquel Grazina
    Centro Química Estrutural, Instituto Superior Técnico UTL, Av Rovisco Pais, 1049 001 Lisboa, Portugal
    J Hazard Mater 186:1902-8. 2011
    ..These functionalized supports also showed capacity to be regenerated and reused. Thus, there are good perspectives for potential environmental and medical applications of these new metal sorbents...
  18. ncbi A gallium complex with a new tripodal tris-hydroxypyridinone for potential nuclear diagnostic imaging: solution and in vivo studies of 67Ga-labeled species
    Silvia Chaves
    Centro de Quimica Estrutural, Instituto Superior Técnico UTL, 1049 001 Lisboa, Portugal
    J Inorg Biochem 105:31-8. 2011
    ..These results indicate good perspectives for potential application of extrafunctionalized analogues in radiodiagnostic techniques...
  19. ncbi Complexes of hydroxy(thio)pyrone and hydroxy(thio)pyridinone with Zn(II) and Mo(VI). Thermodynamic stability and insulin-mimetic activity
    Silvia Chaves
    Centro de Quimica Estrutural, Instituto Superior Tecnico, Av Rovisco Pais 1, 1049 001 Lisboa, Portugal
    Metallomics 2:220-7. 2010
    ..Hence, these preliminary studies indicate that the Zn(thiomaltol)? complex can be considered a potential drug candidate for treatment of diabetes mellitus, upon in vivo evaluations...
  20. ncbi Bifunctional phenolic-choline conjugates as anti-oxidants and acetylcholinesterase inhibitors
    Jaroslav Sebestik
    Centro de Quimica Estrutural, Instituto Superior Tecnico, Av Rovisco Pais 1, 1049 001 Lisboa, Portugal
    J Enzyme Inhib Med Chem 26:485-97. 2011
    ....