Hengmiao Cheng

Summary

Affiliation: Pfizer Global Research and Development
Country: USA

Publications

  1. doi request reprint Recent progress on third generation covalent EGFR inhibitors
    Hengmiao Cheng
    Oncology Medicinal Chemistry, La Jolla Laboratories, Pfizer Worldwide Research and Development, 10770 Science Center Drive, San Diego, CA 92121, United States Electronic address
    Bioorg Med Chem Lett 26:1861-8. 2016
  2. doi request reprint Structure-based design, SAR analysis and antitumor activity of PI3K/mTOR dual inhibitors from 4-methylpyridopyrimidinone series
    Hengmiao Cheng
    Cancer Chemistry, Pfizer Worldwide Research and Development, La Jolla Laboratories, 10770 Science Center Drive, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 23:2787-92. 2013
  3. doi request reprint The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors
    Hengmiao Cheng
    Pfizer Global Research and Development, La Jolla Labs, 10770 Science Center Drive, San Diego, CA 92121, United States
    Bioorg Med Chem Lett 20:2897-902. 2010
  4. ncbi request reprint Synthesis and SAR of heteroaryl-phenyl-substituted pyrazole derivatives as highly selective and potent canine COX-2 inhibitors
    Hengmiao Cheng
    Veterinary Medicine Research and Development Pfizer Inc, Groton, CT 06340, USA
    Bioorg Med Chem Lett 16:2076-80. 2006
  5. doi request reprint Comparative structure-activity relationship studies of 1-(5-methylsulfonylpyrid-2-yl)-5-alkyl and (hetero)aryl triazoles and pyrazoles in canine COX inhibition
    Subas M Sakya
    Veterinary Medicine Research and Development Pfizer Inc, Groton, CT 06340, USA
    Bioorg Med Chem Lett 18:1042-5. 2008
  6. ncbi request reprint 5-Heteroatom substituted pyrazoles as canine COX-2 inhibitors. Part III: molecular modeling studies on binding contribution of 1-(5-methylsulfonyl)pyrid-2-yl and 4-nitrile
    Subas M Sakya
    Veterinary Medicine Research and Development, Pfizer Inc, Groton, CT 06340, USA
    Bioorg Med Chem Lett 17:1067-72. 2007
  7. ncbi request reprint 5-Heteroatom-substituted pyrazoles as canine COX-2 inhibitors: Part 2. Structure-activity relationship studies of 5-alkylethers and 5-thioethers
    Subas M Sakya
    Veterinary Medicine Research and Development, Pfizer Inc, Groton, CT 06340, USA
    Bioorg Med Chem Lett 16:1202-6. 2006
  8. doi request reprint Design and synthesis of a novel pyrrolidinyl pyrido pyrimidinone derivative as a potent inhibitor of PI3Kα and mTOR
    Phuong T Le
    Cancer Chemistry, Pfizer Worldwide Research and Development, La Jolla Laboratories, Pfizer Inc, La Jolla, CA 92121, United States
    Bioorg Med Chem Lett 22:5098-103. 2012
  9. ncbi request reprint Azalide 3,6-ketals: antibacterial activity and structure-activity relationships of aryl and hetero aryl substituted analogues
    Subas M Sakya
    Veterinary Medicine Research and Development, Pfizer Inc, Groton, CT 06340, USA
    Bioorg Med Chem Lett 13:1373-5. 2003
  10. doi request reprint PF-04691502, a potent and selective oral inhibitor of PI3K and mTOR kinases with antitumor activity
    Jing Yuan
    Oncology Research Unit, Pfizer Worldwide Research and Development, La Jolla Laboratories, San Diego, CA 92121, USA
    Mol Cancer Ther 10:2189-99. 2011

Collaborators

Detail Information

Publications22

  1. doi request reprint Recent progress on third generation covalent EGFR inhibitors
    Hengmiao Cheng
    Oncology Medicinal Chemistry, La Jolla Laboratories, Pfizer Worldwide Research and Development, 10770 Science Center Drive, San Diego, CA 92121, United States Electronic address
    Bioorg Med Chem Lett 26:1861-8. 2016
    ..This review provides an overview of the third generation drugs currently in clinical trials and also encompasses novel methodologies developed to discover third generation covalent EGFR drugs. ..
  2. doi request reprint Structure-based design, SAR analysis and antitumor activity of PI3K/mTOR dual inhibitors from 4-methylpyridopyrimidinone series
    Hengmiao Cheng
    Cancer Chemistry, Pfizer Worldwide Research and Development, La Jolla Laboratories, 10770 Science Center Drive, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 23:2787-92. 2013
    ..This paper discusses structure-based drug design, SAR and antitumor activity of the MPP derivatives with a terminal alcohol, a carboxylic acid or a carboxyl amide...
  3. doi request reprint The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors
    Hengmiao Cheng
    Pfizer Global Research and Development, La Jolla Labs, 10770 Science Center Drive, San Diego, CA 92121, United States
    Bioorg Med Chem Lett 20:2897-902. 2010
    ..In an in vivo assay, PF-877423 inhibited the conversion of cortisone to cortisol. Structure guided optimization effort yielded potent and stable 11beta-HSD1 selective inhibitor 42...
  4. ncbi request reprint Synthesis and SAR of heteroaryl-phenyl-substituted pyrazole derivatives as highly selective and potent canine COX-2 inhibitors
    Hengmiao Cheng
    Veterinary Medicine Research and Development Pfizer Inc, Groton, CT 06340, USA
    Bioorg Med Chem Lett 16:2076-80. 2006
    ....
  5. doi request reprint Comparative structure-activity relationship studies of 1-(5-methylsulfonylpyrid-2-yl)-5-alkyl and (hetero)aryl triazoles and pyrazoles in canine COX inhibition
    Subas M Sakya
    Veterinary Medicine Research and Development Pfizer Inc, Groton, CT 06340, USA
    Bioorg Med Chem Lett 18:1042-5. 2008
    ..Both series are quite potent and selective in the canine whole blood (CWB) COX-2 assay, suggesting the increased binding contribution of the hydrophobic side chains...
  6. ncbi request reprint 5-Heteroatom substituted pyrazoles as canine COX-2 inhibitors. Part III: molecular modeling studies on binding contribution of 1-(5-methylsulfonyl)pyrid-2-yl and 4-nitrile
    Subas M Sakya
    Veterinary Medicine Research and Development, Pfizer Inc, Groton, CT 06340, USA
    Bioorg Med Chem Lett 17:1067-72. 2007
    ..In addition, our model suggests a potential contribution from hydrogen bonding of the pyridyl nitrogen to Tyr 355 for the increased activity over the phenyl sulfone analogs...
  7. ncbi request reprint 5-Heteroatom-substituted pyrazoles as canine COX-2 inhibitors: Part 2. Structure-activity relationship studies of 5-alkylethers and 5-thioethers
    Subas M Sakya
    Veterinary Medicine Research and Development, Pfizer Inc, Groton, CT 06340, USA
    Bioorg Med Chem Lett 16:1202-6. 2006
    ..The 4-cyano-5-alkyl ethers were found to have excellent potency and selectivity, whereas the 5-thioethers were potent but less selective than the ether analogs in a canine whole blood (CWB) COX-2 assay...
  8. doi request reprint Design and synthesis of a novel pyrrolidinyl pyrido pyrimidinone derivative as a potent inhibitor of PI3Kα and mTOR
    Phuong T Le
    Cancer Chemistry, Pfizer Worldwide Research and Development, La Jolla Laboratories, Pfizer Inc, La Jolla, CA 92121, United States
    Bioorg Med Chem Lett 22:5098-103. 2012
    ..Synthesis and profile of 1, a PI3Kα/mTOR dual inhibitor, is highlighted...
  9. ncbi request reprint Azalide 3,6-ketals: antibacterial activity and structure-activity relationships of aryl and hetero aryl substituted analogues
    Subas M Sakya
    Veterinary Medicine Research and Development, Pfizer Inc, Groton, CT 06340, USA
    Bioorg Med Chem Lett 13:1373-5. 2003
    ....
  10. doi request reprint PF-04691502, a potent and selective oral inhibitor of PI3K and mTOR kinases with antitumor activity
    Jing Yuan
    Oncology Research Unit, Pfizer Worldwide Research and Development, La Jolla Laboratories, San Diego, CA 92121, USA
    Mol Cancer Ther 10:2189-99. 2011
    ..In summary, PF-04691502 is a potent dual PI3K/mTOR inhibitor with broad antitumor activity. PF-04691502 has entered phase I clinical trials...
  11. ncbi request reprint 5-heteroatom substituted pyrazoles as canine COX-2 inhibitors. Part 1: Structure-activity relationship studies of 5-alkylamino pyrazoles and discovery of a potent, selective, and orally active analog
    Subas M Sakya
    Veterinary Medicine Research and Development Pfizer Inc, Groton, CT 06340, USA
    Bioorg Med Chem Lett 16:288-92. 2006
    ..The studies led to the identification of 2e as lead with potent in vitro activity, selectivity, and in vivo activity in dogs and cats...
  12. ncbi request reprint In vitro and in vivo profile of 2-(3-di-fluoromethyl-5-phenylpyrazol-1-yl)-5-methanesulfonylpyridine, a potent, selective, and orally active canine COX-2 inhibitor
    Jin Li
    Pfizer Inc, Groton, CT 06340, USA
    Bioorg Med Chem 13:1805-9. 2005
    ..This novel COX-2 inhibitor also showed a good pharmacokinetic profile (pk) following oral (po), intravenous (iv), and subcutaneous (sc) dosing and demonstrated excellent in vivo efficacy in a canine synovitis model...
  13. ncbi request reprint Discovery of potent and orally active MTP inhibitors as potential anti-obesity agents
    Jin Li
    Pfizer Inc, Groton, CT 06340, USA
    Bioorg Med Chem Lett 16:3039-42. 2006
    ..We have successfully identified a number of novel MTP inhibitors with single digit nanomolar potency. Analogues 10aq and 10dq demonstrated in vivo efficacy in a murine gut retention assay...
  14. doi request reprint Quinazolines with intra-molecular hydrogen bonding scaffold (iMHBS) as PI3K/mTOR dual inhibitors
    Kevin K C Liu
    Pfizer Global Research and Development, Chemistry Department, 10770 Science Center Drive, La Jolla, CA 92120, USA
    Bioorg Med Chem Lett 21:1270-4. 2011
    ..In addition, a novel synthetic route was developed for these analogs...
  15. ncbi request reprint Discovery of a novel class of exquisitely selective mesenchymal-epithelial transition factor (c-MET) protein kinase inhibitors and identification of the clinical candidate 2-(4-(1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-y
    J Jean Cui
    La Jolla Laboratories, Pfizer Worldwide Research and Development, 10770 Science Center Drive, San Diego, California 92121, USA
    J Med Chem 55:8091-109. 2012
    ..2 demonstrated effective tumor growth inhibition in c-MET dependent tumor models with good oral PK properties and an acceptable safety profile in preclinical studies. 2 progressed to clinical evaluation in a Phase I oncology setting...
  16. ncbi request reprint Synthesis and activity of a novel class of tribasic macrocyclic antibiotics: the triamilides
    Michael A Letavic
    Pfizer Global Research and Development, Groton Laboratories, Eastern Point Road, Groton, CT 06340, USA
    Bioorg Med Chem Lett 12:2771-4. 2002
    ..The effect of substitution and stereochemistry on the in vivo activity in a murine model of respiratory infection is also described...
  17. doi request reprint 4-methylpteridinones as orally active and selective PI3K/mTOR dual inhibitors
    Kevin K C Liu
    Pfizer Global Research and Development, Chemistry Department, La Jolla, CA 92120, USA
    Bioorg Med Chem Lett 20:6096-9. 2010
    ..This series of compounds were further optimized to improve their potency against PI3Kα and mTOR. Finally, orally active compounds with improved solubility and robust in vivo efficacy in tumor growth inhibition were identified as well...
  18. doi request reprint N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1: strategies to eliminate reactive metabolites
    Sajiv K Nair
    Medicinal Chemistry, Pfizer Global R and D, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 23:2344-8. 2013
    ....
  19. ncbi request reprint Targeting the mTOR pathway in tumor malignancy
    Hengmiao Cheng
    Pfizer Worldwide Research and Development, 10724 Science Center Drive, San Diego, CA 92121, USA
    Curr Cancer Drug Targets 13:267-77. 2013
    ..Here we discuss the mechanism of mTOR regulation in tumor malignancy through a variety of signaling pathways and the potential of mTOR inhibitors for the treatment of cancer...
  20. doi request reprint Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants
    Hengmiao Cheng
    La Jolla Laboratories, Pfizer Worldwide Research and Development, 10770 Science Center Drive, San Diego, California 92121, United States
    J Med Chem 59:2005-24. 2016
    ....
  21. ncbi request reprint Synthesis and SAR of azalide 3,6-ketal aromatic derivatives as potent Gram-positive and Gram-negative antibacterial agents
    Hengmiao Cheng
    Pfizer Global Research and Development, Groton Laboratories, Groton, CT 06340, USA
    Bioorg Med Chem Lett 12:2431-4. 2002
    ..The aromatic derivatives of the azalide 3,6-ketals demonstrated potent antibacterial activities against both Gram-positive and Gram-negative bacteria...
  22. doi request reprint In vivo evaluation of 11beta-hydroxysteroid dehydrogenase activity in the rabbit eye
    Scott Anderson
    Pfizer Global R and D La Jolla, San Diego, CA 92121, USA
    J Ocul Pharmacol Ther 25:215-22. 2009
    ....