2. Academic Validation
  3. Synthesis of tricyclic fused coumarin sulfonates and their inhibitory effects on LPS-induced nitric oxide and PGE2 productions in RAW 264.7 macrophages

Synthesis of tricyclic fused coumarin sulfonates and their inhibitory effects on LPS-induced nitric oxide and PGE2 productions in RAW 264.7 macrophages

  • Bioorg Med Chem Lett. 2014 Jan 15;24(2):571-5. doi: 10.1016/j.bmcl.2013.12.018.
Hyeon-Lok Jang 1,  Mohammed I El-Gamal 2,  Hye-Eun Choi 3,  Ho-Yeong Choi 1,  Kyung-Tae Lee 4,  Chang-Hyun Oh 5
Affiliations

Affiliations

  • 1 Korean Medical School, Kyung Hee University, Hoegi-dong, Dongdaemoon-ku, Seoul 130-701, Republic of Korea.
  • 2 Center for Biomaterials, Korea Institute of Science and Technology (KIST), PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea; Department of Biomolecular Science, University of Science and Technology (UST), 113 Gwahangno, Yuseong-gu, Daejeon 305-333, Republic of Korea; Department of Medicinal Chemistry, Faculty of Pharmacy, University of Mansoura, Mansoura 35516, Egypt.
  • 3 Department of Pharmaceutical Biochemistry, Department of Life and Nanopharmaceutical Science, College of Pharmacy, Kyung Hee University, 1 Hoegi-dong, Dongdaemun-gu, Seoul 130-701, Republic of Korea.
  • 4 Department of Pharmaceutical Biochemistry, Department of Life and Nanopharmaceutical Science, College of Pharmacy, Kyung Hee University, 1 Hoegi-dong, Dongdaemun-gu, Seoul 130-701, Republic of Korea. Electronic address: ktlee@khu.ac.kr.
  • 5 Center for Biomaterials, Korea Institute of Science and Technology (KIST), PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea; Department of Biomolecular Science, University of Science and Technology (UST), 113 Gwahangno, Yuseong-gu, Daejeon 305-333, Republic of Korea. Electronic address: choh@kist.re.kr.
PMID: 24360561 DOI: 10.1016/j.bmcl.2013.12.018
Abstract

The regulations of NO and PGE2 productions are research topics of interest in the field of antiinflammatory drug development. In the present study, a series of tricyclic fused coumarin sulfonate derivatives was synthesized and evaluated for their abilities to inhibit NO and PGE2 productions in LPS-induced RAW 264.7 macrophages. Among all the target compounds, compound 1g possessing p-(trifluoromethyl)phenyl and fused cycloheptane moieties showed the highest inhibitory effects on NO and PGE2 productions. Compound 1g not only inhibited COX-2 activity but also reduced expressions of COX-2 and iNOS. Furthermore, ADME profiling showed that compounds 1g, 1j, 1m, and 1n are estimated to be orally bioavailable.

Keywords

Antiinflammatory; Coumarin; Nitric oxide; PGE(2); Sulfonate; Tricyclic fused coumarin.

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