Design and synthesis of novel iminothiazinylbutadienols and divinylpyrimidinethiones as ARE inducers

被引：8

作者：

Chen, Lin ^{[1
]}

Magesh, Sadagopan ^{[1
]}

Wang, Hong ^{[2
]}

Yang, Chung S. ^{[2
,5
,6
]}

Ah-Ng Tony Kong ^{[3
,5
,6
]}

Hu, Longqin ^{[1
,4
,5
,6
]}

机构：

[1] Rutgers State Univ, Ernest Mario Sch Pharm, Dept Med Chem, Piscataway, NJ 08854 USA

[2] Rutgers State Univ, Ernest Mario Sch Pharm, Dept Biol Chem, Piscataway, NJ 08854 USA

[3] Rutgers State Univ, Ernest Mario Sch Pharm, Dept Pharmaceut, Piscataway, NJ 08854 USA

[4] Shanxi Med Univ, Sch Pharmaceut Sci, Taiyuan 030001, Peoples R China

[5] Canc Inst New Jersey, New Brunswick, NJ 08901 USA

[6] Rutgers State Univ, Ernest Mario Sch Pharm, Ctr Canc Prevent Res, Piscataway, NJ 08854 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 03期

基金：

美国国家卫生研究院;

关键词：

Curcumin; Iminothiazinylbutadienols; Divinylpyrimidinethiones; Anti-inflammatory agents; ARE induction; CURCUMIN ANALOGS; ANTIINFLAMMATORY PROPERTIES; NATURAL CURCUMINOIDS; HEME OXYGENASE-1; CANCER; ANTIOXIDANT; INHIBITION; STABILITY; AGENTS; ANGIOGENESIS;

D O I：

10.1016/j.bmcl.2013.12.072

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

Novel iminothiazinylbutadienols and divinylpyrimidinethiones were designed and synthesized as analogues of curcumin with its diketone moiety masked as a heterocyclic adduct with thiourea. The chemical stability of these novel heterocyclic compounds was improved as compared to curcumin. They exhibit longer half-lives and do not react with nucleophilic thiols under physiological conditions. In an ARE-luciferase reporter assay, some of these new curcumin analogues are more effective ARE activators than curcumin and isothiocyanates. (C) 2014 Elsevier Ltd. All rights reserved.

引用

页码：940 / 943

页数：4

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