Synthesis, cytotoxicity, and structure-activity relationship (SAR) studies of andrographolide analogues as anti-cancer agent.

Das B; Chowdhury C; Kumar D; Sen R; Roy R; Das P; Chatterjee M

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Synthesis, cytotoxicity, and structure-activity relationship (SAR) studies of andrographolide analogues as anti-cancer agent.

机译：穿心莲内酯类似物作为抗癌药的合成，细胞毒性和结构活性关系（SAR）研究。

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A series of analogues of andrographolide, prepared through chemo-selective functionalization at C14 hydroxy, have been evaluated for in vitro cytotoxicities against human leukemic cell lines. Two of the analogues (6a, 9b) exhibited significant potency. Preliminary studies on structure-activity relationship (SAR) revealed that the alpha-alkylidene-gamma-butyrolactone moiety of andrographolide played a major role in the activity profile. The structures of the analogues were established through spectroscopic and analytical data.

机译：已通过在C14羟基处进行化学选择性官能化制备了一系列穿心莲内酯类似物，以评估其对人白血病细胞系的体外细胞毒性。其中两个类似物（6a，9b）表现出显着的效力。对结构-活性关系（SAR）的初步研究表明，穿心莲内酯的α-亚烷基-γ-丁内酯部分在活性谱中起主要作用。通过光谱和分析数据确定类似物的结构。

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《Bioorganic and Medicinal Chemistry Letters》 |2010年第23期|共4页
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Das B; Chowdhury C; Kumar D; Sen R; Roy R; Das P; Chatterjee M;
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1. Synthesis, cytotoxicity, and structure-activity relationship (SAR) studies of andrographolide analogues as anti-cancer agent. [J] . Das B, Chowdhury C, Kumar D, Bioorganic and Medicinal Chemistry Letters . 2010,第23期

机译：穿心莲内酯类似物作为抗癌药的合成，细胞毒性和结构活性关系（SAR）研究。
2. Aqua mediated synthesis of 2-amino-6-benzothiazol-2-ylsulfanyl-chromenes and its in vitro study, explanation of the structure-activity relationships (SARs) as antibacterial agent. [J] . Kidwai M, Poddar R, Bhardwaj S, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2010,第11期

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3. Aqua mediated synthesis of 2-amino-6-benzothiazol-2-ylsulfanyl-chromenes and its in vitro study, explanation of the structure-activity relationships (SARs) as antibacterial agent. [J] . Kidwai M, Poddar R, Bhardwaj S, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2010,第11期

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Synthesis, cytotoxicity, and structure-activity relationship (SAR) studies of andrographolide analogues as anti-cancer agent.

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