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 Chou

Research output: Contribution to journalArticle

4 Citations (Scopus)


Synthetic thalidomide analogues (compounds 1-35), 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.

Original languageEnglish
Pages (from-to)953-963
Number of pages11
JournalMedicinal Chemistry Research
Issue number7
Publication statusPublished - Jul 2012



  • Nitric oxide synthase inhibitors
  • Thalidomide
  • Thalidomide analogues

ASJC Scopus subject areas

  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Organic Chemistry

Cite this