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

研究成果: 雜誌貢獻文章

4 引文 (Scopus)

摘要

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.

原文英語
頁(從 - 到)953-963
頁數11
期刊Medicinal Chemistry Research
21
發行號7
DOIs
出版狀態已發佈 - 七月 2012

指紋

Thalidomide
Nitric Oxide Synthase Type II
Bioactivity
Cells
HL-60 Cells
Carcinoma
Cell Line
Myeloid Leukemia
Therapeutic Uses
Myeloid Cells
Larynx
Nitric Oxide Synthase
Neoplasms
Stomach
Nitric Oxide
Incidence
Therapeutics

ASJC Scopus subject areas

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

引用此文

Study on synthesis of thalidomide analogues and their bioactivities; Inhibition on iNOS pathway and cytotoxic effects. / Yeh, Chao Bin; Lin, Pen Yuan; Hwang, Jin Ming; Su, Chi Jung; Yeh, Ying Tung; Yang, Shun Fa; Chou, Ming Chih.

於: Medicinal Chemistry Research, 卷 21, 編號 7, 07.2012, p. 953-963.

研究成果: 雜誌貢獻文章

Yeh, Chao Bin ; Lin, Pen Yuan ; Hwang, Jin Ming ; Su, Chi Jung ; Yeh, Ying Tung ; Yang, Shun Fa ; Chou, Ming Chih. / Study on synthesis of thalidomide analogues and their bioactivities; Inhibition on iNOS pathway and cytotoxic effects. 於: Medicinal Chemistry Research. 2012 ; 卷 21, 編號 7. 頁 953-963.
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abstract = "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.",
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AU - Yang, Shun Fa

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