Conformationally constrained analogues of diacylglycerol (DAG). Effect on protein kinase C (PK-C) binding by the isosteric replacement of sn-1 and sn-2 esters in …

…, J Lee, NE Lewin, LV Pearce, PM Blumberg…

Index: Kang, Ji-Hye; Chung, Hye-Eun; Kim, Su Yeon; Kim, Yerim; Lee, Jeewoo; Lewin, Nancy E.; Pearce, Larry V.; Blumberg, Peter M.; Marquez, Victor E. Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 12 p. 2529 - 2539

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Citation Number: 20

Abstract

In order to determine the importance of the two ester pharmacophores in high affinity, conformationally constrained DAG-lactones (Lac-1–5) as PK-C ligands, we have independently replaced the sn-1 and sn-2 carbonyl esters in these compounds by ketone (2, 10, 11), amide (3, 25–28), and hydroxyl (12, 13) isosteres. Although the ketone analogue of the sn-1 ester (2) exhibited comparable activity to the parent Lac-1 when taking into ...

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