Qingzhong Hu

Summary

Affiliation: Saarland University
Country: Germany

Publications

  1. 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
  2. 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
  3. 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
  4. 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
  5. doi 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
  6. 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
  7. 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
  8. 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
  9. 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
  10. 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

Collaborators

Detail Information

Publications10

  1. 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)...
  2. 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...
  3. 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...
  4. 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...
  5. doi 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...
  6. 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...
  7. 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
    ....
  8. 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. ..
  9. 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. ..
  10. 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
    ....