Medicinal Chemistry Research

, Volume 21, Issue 7, pp 953–963 | Cite as

Study on synthesis of thalidomide analogues and their bioactivities; inhibition on iNOS pathway and cytotoxic effects

  • Chao-Bin Yeh
  • Pen-Yuan Lin
  • Jin-Ming Hwang
  • Chi-Jung Su
  • Ying-Tung Yeh
  • Shun-Fa Yang
  • Ming-Chih ChouEmail author
Original Research


Synthetic thalidomide analogues (compounds 135), including phenylphthalimide, pyridylphthalimide, aminobenzylphthalimide, and diphenylazophthalimide, were tested for their cytotoxic effects on human cancer cell lines Hep2 (Human Larynx Carcinoma Cells), HL-60 (Human Myeloid Leukemia Cells), NUGC (Human Gastric Carcinoma Cells), and HONE-1 (Human Nasopharyngeal Carcinoma Cells) because the incidence rate is more prominent in Asian countries than in Western countries. Compounds 17, 27, 28, and 35 were found to have antitumor activity in Hep2 and HL-60 cell lines. Compounds 2, 4, 15, 17, 19, 20, 23, and 27 can inhibit nitric oxide (NO) synthase activity by more than 90%. These thalidomide analogues were found to be potent inducible nitric oxide synthase (iNOS) inhibitors, and the iNOS inhibiting potential of compounds 17 and 27 might be an advantage for anticancer therapy. In conclusion, inhibition of NO synthesis is a new development in cancer therapy for now and in the future. We modified the structures of the thalidomide analogues to have a stronger anticancer effect and a good therapeutic effect.


Thalidomide Thalidomide analogues Nitric oxide synthase inhibitors 



We would like to thank Professor Jer-Yuh Liu from the Graduate Institute of Cancer Biology, College of Medicine, China Medical University for his consultation and invaluable advice on this paper. This study was supported by a research grant from Chung Shan Medical University Hospital, Taiwan (CSH-2011-C-001).


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Copyright information

© Springer Science+Business Media, LLC 2011

Authors and Affiliations

  • Chao-Bin Yeh
    • 1
    • 2
    • 3
  • Pen-Yuan Lin
    • 4
  • Jin-Ming Hwang
    • 5
  • Chi-Jung Su
    • 5
  • Ying-Tung Yeh
    • 6
  • Shun-Fa Yang
    • 2
    • 7
  • Ming-Chih Chou
    • 1
    • 2
    • 8
    Email author
  1. 1.School of MedicineChung Shan Medical UniversityTaichungTaiwan
  2. 2.Institute of MedicineChung Shan Medical UniversityTaichungTaiwan
  3. 3.Department of Emergency MedicineChung Shan Medical University HospitalTaichungTaiwan
  4. 4.School of PharmacyTaipei Medical UniversityTaipeiTaiwan
  5. 5.School of Apply ChemicalChung Shan Medical UniversityTaichungTaiwan
  6. 6.School of DentistryChung Shan Medical UniversityTaichungTaiwan
  7. 7.Department of Medical ResearchChung Shan Medical University HospitalTaichungTaiwan
  8. 8.Department of SurgeryChung Shan Medical University HospitalTaichungTaiwan

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