Earticle

초록

영어

Prostaglandins have a short life in vivo because they are metabolized rapidly by oxidation to 15-ketoprostaglandins catalyzed by a cytosolic enzyme known as NAD+-dependent 15-hydroxyprostaglandin dehydrogenase (15-PGDH). Previously, CT-8, a thiazolidinedione analogue, was found to be a potent inhibitor of 15-PGDH. Structure-activity analysis indicated
that the N-methylation of thiazolidine-2,4-dione, CT-8, abolished the inhibitory activity, whereas the introduction of an ethyl hydroxyl group at amine in CT-8 still had a good inhibitory effect. Based on the structures of the thiazolidinediones analogues and inhibitory activity, a range of
benzylidene thiazolidinedione derivatives were synthesized with different substituents on the phenyl ring and their inhibitory activity was evaluated. Replacement of the cyclohexylethyl group of CT-8 with the hetero 5-member ring increased the inhibitory potency. However, replacement
of the cyclohexylethyl group with a hetero 6-member ring decreased the inhibitory potency significantly. It was found that compound 2(5-(4-(2-(thiophen-2-yl)ethoxy)benzylidene)thiazolidine-2,4-dione) was the most potent inhibitor that was effective in the nanomolar range.

키워드

저자

• Hoon CHO [ Dept. of Polymer Science & Engineering, Research Center for Resistant Cells, Gwangju 501-759, Korea. ]
• Ying WU [ Dept. of Polymer Science & Engineering, Chosun University, Gwangju 501-759, Korea. ]
• Le Thi HANG [ Dept. of Polymer Science & Engineering, Chosun University, Gwangju 501-759, Korea. ]

참고문헌

발행기관

간행물

표지보기 관심저널 등록

• 간행물명

  한국생물공학회 학술대회

• 간기

  반년간

• 수록기간

  1985~2013

• 십진분류

  KDC 476 DDC 576