Qingzhong Hu

Summary

Affiliation: Saarland University
Country: Germany

Publications

  1. pmc 3-Pyridyl substituted aliphatic cycles as CYP11B2 inhibitors: aromaticity abolishment of the core significantly increased selectivity over CYP1A2
    Lina Yin
    Pharmaceutical and Medicinal Chemistry, Saarland University and Helmholtz Institute for Pharmaceutical Research Saarland HIPS, Saarbrucken, Germany
    PLoS ONE 7:e48048. 2012
  2. doi request reprint Selective dual inhibitors of CYP19 and CYP11B2: targeting cardiovascular diseases hiding in the shadow of breast cancer
    Qingzhong Hu
    Pharmaceutical and Medicinal Chemistry, Saarland University and Helmholtz Institute for Pharmaceutical Research Saarland HIPS, Campus C2 3, P O Box 151150, D 66123 Saarbrucken, Germany
    J Med Chem 55:7080-9. 2012
  3. doi request reprint CYP17 inhibitors. Annulations of additional rings in methylene imidazole substituted biphenyls: synthesis, biological evaluation and molecular modelling
    Mariano A E Pinto-Bazurco Mendieta
    Pharmaceutical and Medicinal Chemistry, Saarland University, Saarbrucken, Germany
    Arch Pharm (Weinheim) 341:597-609. 2008
  4. doi request reprint Isopropylidene substitution increases activity and selectivity of biphenylmethylene 4-pyridine type CYP17 inhibitors
    Qingzhong Hu
    Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C23, D 66123 Saarbrucken, Germany
    J Med Chem 53:5049-53. 2010
  5. ncbi request reprint Synthesis, biological evaluation, and molecular modeling studies of methylene imidazole substituted biaryls as inhibitors of human 17alpha-hydroxylase-17,20-lyase (CYP17)--part II: Core rigidification and influence of substituents at the methylene bridge
    Qingzhong Hu
    Pharmaceutical and Medicinal Chemistry, Saarland University, PO Box 151150, D 66041 Saarbrucken, Germany
    Bioorg Med Chem 16:7715-27. 2008
  6. doi request reprint Novel CYP17 inhibitors: synthesis, biological evaluation, structure-activity relationships and modelling of methoxy- and hydroxy-substituted methyleneimidazolyl biphenyls
    Ulrike E Hille
    Pharmaceutical and Medicinal Chemistry, Saarland University, Saarbrucken, Germany
    Eur J Med Chem 44:2765-75. 2009
  7. ncbi request reprint The role of fluorine substitution in biphenyl methylene imidazole-type CYP17 inhibitors for the treatment of prostate carcinoma
    Qingzhong Hu
    Pharmaceutical and Medicinal Chemistry, Saarland University, PO Box 151150 and Helmholtz Institute for Pharmaceutical Research, Saarland HIPS, 66041 Saarbrucken, Germany
    ChemMedChem 5:899-910. 2010
  8. doi request reprint Replacement of imidazolyl by pyridyl in biphenylmethylenes results in selective CYP17 and dual CYP17/CYP11B1 inhibitors for the treatment of prostate cancer
    Qingzhong Hu
    Pharmaceutical and Medicinal Chemistry and Helmholtz Institute for Pharmaceutical Research Saarland HIPS, Saarland University, Saarbrucken, Germany
    J Med Chem 53:5749-58. 2010
  9. doi request reprint Novel imidazol-1-ylmethyl substituted 1,2,5,6-tetrahydropyrrolo[3,2,1-ij]quinolin-4-ones as potent and selective CYP11B1 inhibitors for the treatment of Cushing's syndrome
    Lina Yin
    Pharmaceutical and Medicinal Chemistry, Saarland University and Helmholtz Institute for Pharmaceutical Research Saarland HIPS, Campus C2 3, D 66123 Saarbrucken, Germany
    J Med Chem 55:6629-33. 2012
  10. doi request reprint Tetrahydropyrroloquinolinone type dual inhibitors of aromatase/aldosterone synthase as a novel strategy for breast cancer patients with elevated cardiovascular risks
    Lina Yin
    Pharmaceutical and Medicinal Chemistry, Saarland University and Helmholtz Institute for Pharmaceutical Research Saarland HIPS, Campus C2 3, D 66123 Saarbrucken, Germany
    J Med Chem 56:460-70. 2013

Collaborators

  • Rolf W Hartmann
  • Sureyya Olgen
  • Andrea Cavalli
  • Uli Kazmaier
  • Maurizio Recanatini
  • Lina Yin
  • Mariano A E Pinto-Bazurco Mendieta
  • Ulrike E Hille
  • Juliette Emmerich
  • Thomas Lauterbach
  • Ursula Müller-Vieira
  • Matthias Negri
  • Carsten Jagusch
  • Sebastian J Krug
  • Marc Bartels
  • Kerstin Jahn-Hoffmann
  • Dirk Schmidt
  • Edward Metzger
  • Amjad Ali
  • Michael Man Chu Lo
  • Nina Hanke
  • Matthias Engel
  • Simon Lucas
  • Frauke Maurer
  • Carsten Vock
  • Barbara Rodenwaldt

Detail Information

Publications18

  1. pmc 3-Pyridyl substituted aliphatic cycles as CYP11B2 inhibitors: aromaticity abolishment of the core significantly increased selectivity over CYP1A2
    Lina Yin
    Pharmaceutical and Medicinal Chemistry, Saarland University and Helmholtz Institute for Pharmaceutical Research Saarland HIPS, Saarbrucken, Germany
    PLoS ONE 7:e48048. 2012
    ..The design conception demonstrated in this study can be helpful in the optimization of CYP inhibitor drugs regarding CYP1A2 selectivity...
  2. doi request reprint Selective dual inhibitors of CYP19 and CYP11B2: targeting cardiovascular diseases hiding in the shadow of breast cancer
    Qingzhong Hu
    Pharmaceutical and Medicinal Chemistry, Saarland University and Helmholtz Institute for Pharmaceutical Research Saarland HIPS, Campus C2 3, P O Box 151150, D 66123 Saarbrucken, Germany
    J Med Chem 55:7080-9. 2012
    ..These compounds showed also good selectivity toward CYP11B1 (selectivity factors (IC(50 CYP11B1)/IC(50 CYP11B2)) around 50) and CYP17 (no inhibition)...
  3. doi request reprint CYP17 inhibitors. Annulations of additional rings in methylene imidazole substituted biphenyls: synthesis, biological evaluation and molecular modelling
    Mariano A E Pinto-Bazurco Mendieta
    Pharmaceutical and Medicinal Chemistry, Saarland University, Saarbrucken, Germany
    Arch Pharm (Weinheim) 341:597-609. 2008
    ..The most interesting compounds were docked into our protein model. They bound into one of the modes which we have previously published. New interaction regions were identified...
  4. doi request reprint Isopropylidene substitution increases activity and selectivity of biphenylmethylene 4-pyridine type CYP17 inhibitors
    Qingzhong Hu
    Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C23, D 66123 Saarbrucken, Germany
    J Med Chem 53:5049-53. 2010
    ....
  5. ncbi request reprint Synthesis, biological evaluation, and molecular modeling studies of methylene imidazole substituted biaryls as inhibitors of human 17alpha-hydroxylase-17,20-lyase (CYP17)--part II: Core rigidification and influence of substituents at the methylene bridge
    Qingzhong Hu
    Pharmaceutical and Medicinal Chemistry, Saarland University, PO Box 151150, D 66041 Saarbrucken, Germany
    Bioorg Med Chem 16:7715-27. 2008
    ..Using our CYP17 homology protein model, docking studies with selected compounds were performed to study possible interactions between inhibitors and amino acid residues of the active site...
  6. doi request reprint Novel CYP17 inhibitors: synthesis, biological evaluation, structure-activity relationships and modelling of methoxy- and hydroxy-substituted methyleneimidazolyl biphenyls
    Ulrike E Hille
    Pharmaceutical and Medicinal Chemistry, Saarland University, Saarbrucken, Germany
    Eur J Med Chem 44:2765-75. 2009
    ..Docking studies using our CYP17 protein model were performed with selected compounds to study the interactions between the inhibitors and the amino acid residues of the active site...
  7. ncbi request reprint The role of fluorine substitution in biphenyl methylene imidazole-type CYP17 inhibitors for the treatment of prostate carcinoma
    Qingzhong Hu
    Pharmaceutical and Medicinal Chemistry, Saarland University, PO Box 151150 and Helmholtz Institute for Pharmaceutical Research, Saarland HIPS, 66041 Saarbrucken, Germany
    ChemMedChem 5:899-910. 2010
    ..The SARs obtained confirm the reliability of the protein model; compound 9 (IC(50)=131 nM) was identified as a strong CYP17 inhibitor, showing potent activity in rat, high bioavailability, and a long plasma half-life: 12.8 h...
  8. doi request reprint Replacement of imidazolyl by pyridyl in biphenylmethylenes results in selective CYP17 and dual CYP17/CYP11B1 inhibitors for the treatment of prostate cancer
    Qingzhong Hu
    Pharmaceutical and Medicinal Chemistry and Helmholtz Institute for Pharmaceutical Research Saarland HIPS, Saarland University, Saarbrucken, Germany
    J Med Chem 53:5749-58. 2010
    ....
  9. doi request reprint Novel imidazol-1-ylmethyl substituted 1,2,5,6-tetrahydropyrrolo[3,2,1-ij]quinolin-4-ones as potent and selective CYP11B1 inhibitors for the treatment of Cushing's syndrome
    Lina Yin
    Pharmaceutical and Medicinal Chemistry, Saarland University and Helmholtz Institute for Pharmaceutical Research Saarland HIPS, Campus C2 3, D 66123 Saarbrucken, Germany
    J Med Chem 55:6629-33. 2012
    ..2 nM) than leads and more selective (SF = 11) than I and metyrapone. Since it also showed potent inhibition of rat CYP11B1 and good selectivity over human CYP17 and CYP19, it is a promising candidate for further development...
  10. doi request reprint Tetrahydropyrroloquinolinone type dual inhibitors of aromatase/aldosterone synthase as a novel strategy for breast cancer patients with elevated cardiovascular risks
    Lina Yin
    Pharmaceutical and Medicinal Chemistry, Saarland University and Helmholtz Institute for Pharmaceutical Research Saarland HIPS, Campus C2 3, D 66123 Saarbrucken, Germany
    J Med Chem 56:460-70. 2013
    ..This compound is considered as a candidate for further evaluation in vivo...
  11. doi request reprint Highly potent and selective nonsteroidal dual inhibitors of CYP17/CYP11B2 for the treatment of prostate cancer to reduce risks of cardiovascular diseases
    Mariano A E Pinto-Bazurco Mendieta
    Pharmaceutical and Medicinal Chemistry, Saarland University and Helmholtz Institute for Pharmaceutical Research Saarland HIPS, Campus C2 3, D 66123 Saarbrucken, Germany
    J Med Chem 56:6101-7. 2013
    ..These compounds are considered as promising candidates for further in vivo evaluation. ..
  12. doi request reprint Cushing's syndrome: development of highly potent and selective CYP11B1 inhibitors of the (pyridylmethyl)pyridine type
    Juliette Emmerich
    Pharmaceutical and Medicinal Chemistry, Saarland University, and Department of Drug Design and Optimization, Helmholtz Institute for Pharmaceutical Research Saarland HIPS, Campus C2 3, 66123 Saarbrucken, Germany
    J Med Chem 56:6022-32. 2013
    ..Investigation of cytotoxicity and inhibition of hepatic CYP2A6 and CYP3A4 showed that 44 fulfills first safety criteria and can be considered for further in vivo evaluation in rats. ..
  13. doi request reprint Hits identified in library screening demonstrate selective CYP17A1 lyase inhibition
    Sebastian J Krug
    Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C2 3, 66123 Saarbrucken, Germany
    J Steroid Biochem Mol Biol 134:75-9. 2013
    ..Hits identified within this novel assay demonstrated selective inhibition of CYP17A1 lyase activity, and thus mark the basis for the development of selective C(17,20)-lyase inhibitors for the treatment of prostate cancer...
  14. ncbi request reprint Novel pyridyl- or isoquinolinyl-substituted indolines and indoles as potent and selective aldosterone synthase inhibitors
    Lina Yin
    Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C2 3, D 66123 Saarbrucken, Germany
    J Med Chem 57:5179-89. 2014
    ..Because of these advantageous profiles, compounds 14 and 23 are considered to be candidates for further in vivo evaluation. ..
  15. pmc Recent progress in pharmaceutical therapies for castration-resistant prostate cancer
    Lina Yin
    Pharmaceutical and Medicinal Chemistry, Saarland University and Helmholtz Institute for Pharmaceutical Research Saarland HIPS, Campus C2 3, Saarbrücken D 66123, Germany
    Int J Mol Sci 14:13958-78. 2013
    ....
  16. ncbi request reprint Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases
    Qingzhong Hu
    Pharmaceutical and Medicinal Chemistry, Saarland University and Helmholtz Institute for Pharmaceutical Research Saarland HIPS, Campus C2 3, D 66123 Saarbrucken, Germany
    J Med Chem 57:5011-22. 2014
    ..Recently, much more selective CYP11B2 inhibitors have been reported, which could be promising drug candidates for the treatment of aldosterone related diseases. ..
  17. ncbi request reprint Synthesis, biological evaluation and molecular modelling studies of methyleneimidazole substituted biaryls as inhibitors of human 17alpha-hydroxylase-17,20-lyase (CYP17). Part I: Heterocyclic modifications of the core structure
    Carsten Jagusch
    Pharmaceutical and Medicinal Chemistry, Saarland University, PO Box 151150, D 66041 Saarbrucken, Germany
    Bioorg Med Chem 16:1992-2010. 2008
    ..5 h vs 1.6 h). Docking studies revealed two new binding modes different from the one of the substrates and steroidal inhibitors...
  18. ncbi request reprint CYP17 inhibitors--abiraterone, C17,20-lyase inhibitors and multi-targeting agents
    Lina Yin
    Department of Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C2 3, D 66123 Saarbrucken, Germany
    Nat Rev Urol 11:32-42. 2014
    ..Some of these strategies-including the drugs orteronel, VT-464 and galeterone--are supported by preclinical data and are being explored in the clinic...