Earticle

초록

영어

Thiazolidinedione analogue, CT-8, has been reported to be a potent inhibitor of human 15-hydroxyprostaglandin dehydrogenase (15-PGDH). In continuing attempts to develop highly potent 15-PGDH inhibitors, a series of thiazolidinedione analogues with different substituents on phenyl rings were synthesized and tested. Of the compounds produced, those in the low nanomolar range were most effective. In particular, introduction of halogen atoms at the phenyl ring of CT-8 greatly improved its inhibitory efficacy. For structure-activity analysis, the effects of adding cyclohexyl with different chain lengths to the hydroxyl groups of 5-(3-substituted-4-hydroxybenzylidene)thiazolidine-2,4-dione were tested. Removal of the methylene group between the cyclohexyl ring and oxygen of 5-(3-substituted-4-(2-cyclohexylethoxy)benzylidene)thiazolidine-2, 4-dione decreased its inhibitory potency. It appears that two methylene groups between the cyclohexyl ring and oxygen of 5-(3-substituted- 4-hydroxybenzylidene)thiazolidine-2,4-dione are optimal for inhibitory activity. The most potent inhibitor of this series of compounds is compound 5, (5-(3-chloro-4-(2-cyclohexylethoxy)benzyl)thiazolidine-2,4-dione), with an IC50 of 0.008 μM.

키워드

저자

• A Ram SONG [ Department of Polymer Science & Engineering, Chosun University, Gwangju 501-759. ]
• Hoon CHO [ Department of Polymer Science & Engineering, Chosun University, Gwangju 501-759. ]

참고문헌

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간행물

표지보기 관심저널 등록

• 간행물명

  한국생물공학회 학술대회

• 간기

  반년간

• 수록기간

  1985~2013

• 십진분류

  KDC 476 DDC 576