Xiaohui He

Publications (4)10.22 Total impact

• Article: Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.

  Baogen Wu, Kelli Kuhen, Truc Ngoc Nguyen, David Ellis, Beth Anaclerio, Xiaohui He, Kunyong Yang, Donald Karanewsky, Hong Yin, Karen Wolff, Kimberly Bieza, Jeremy Caldwell, Yun He
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  ABSTRACT: The synthesis and preliminary structure-activity relationship of a series of pyrrolidinones are described. These pyrrolidinones have been characterized as novel non-nucleoside reverse transcriptase inhibitors (NNRTIs) which are highly potent against wild-type and drug-resistant human immunodeficiency viruses (HIV-1).
  Bioorganic & Medicinal Chemistry Letters 08/2006; 16(13):3430-3. · 2.55 Impact Factor
• Article: Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 2.

  Ha-Soon Choi, Zhicheng Wang, Wendy Richmond, Xiaohui He, Kunyong Yang, Tao Jiang, Donald Karanewsky, Xiang-ju Gu, Vicki Zhou, Yi Liu, Jianwei Che, Christian C Lee, Jeremy Caldwell, Takanori Kanazawa, Ichiro Umemura, Naoko Matsuura, Osamu Ohmori, Toshiyuki Honda, Nathanael Gray, Yun He
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  ABSTRACT: A series of 2-amino-9-aryl-7H-pyrrolo[2,3-d]pyrimidines were designed and synthesized as focal adhesion kinase (FAK) inhibitors using molecular modeling in conjunction with a co-crystal structure. Chemistry was developed to introduce functionality onto the 9-aryl ring, which resulted in the identification of potent FAK inhibitors. In particular, compound 32 possessed single-digit nanomolar IC(50) and represents one of the most potent FAK inhibitors discovered to date.
  Bioorganic & Medicinal Chemistry Letters 06/2006; 16(10):2689-92. · 2.55 Impact Factor
• Article: Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 1.

  Ha-Soon Choi, Zhicheng Wang, Wendy Richmond, Xiaohui He, Kunyong Yang, Tao Jiang, Taebo Sim, Donald Karanewsky, Xiang-ju Gu, Vicki Zhou, Yi Liu, Osamu Ohmori, Jeremy Caldwell, Nathanael Gray, Yun He
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  ABSTRACT: A series of 2-amino-9-aryl-7H-pyrrolo[2,3-d]pyrimidines were designed and synthesized to target focal adhesion kinase (FAK). A number of these pyrrolopyrimides exhibited low micromolar inhibitory activities against focal adhesion kinase, and their preliminary SAR was established via systematic chemical modifications. The 2-amino-9-aryl-7H-pyrrolo[2,3-d]pyrimidines represent a new class of kinase inhibitors.
  Bioorganic & Medicinal Chemistry Letters 05/2006; 16(8):2173-6. · 2.55 Impact Factor
• Article: Identification of novel potent bicyclic peptide deformylase inhibitors.

  Valentina Molteni, Xiaohui He, Juliet Nabakka, Kunyong Yang, Andreas Kreusch, Perry Gordon, Badry Bursulaya, Ian Warner, Tanya Shin, Tanya Biorac, Neil S Ryder, Ron Goldberg, John Doughty, Yun He
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  ABSTRACT: Screening of our compound collection using Staphylococcus aureus Ni-Peptide deformylase (PDF) afforded a very potent PDF inhibitor with an IC(50) in the low nanomolar range but with poor antibacterial activity (MIC). Three-dimensional structural information obtained from Pseudomonas aeruginosa Ni-PDF complexed with the inhibitor suggested the synthesis of a variety of analogues that would maintain high binding affinity while attempting to improve antibacterial activity. Many of the compounds synthesized proved to be excellent PDF-Ni inhibitors and some showed increased antibacterial activity in selected strains.
  Bioorganic & Medicinal Chemistry Letters 04/2004; 14(6):1477-81. · 2.55 Impact Factor