Synthesis of trans-caffeate analogues and their bioactivities against HIV-1 integrase and cancer cell lines.

Xia CN; Li HB; Liu F; Hu WX

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Synthesis of trans-caffeate analogues and their bioactivities against HIV-1 integrase and cancer cell lines.

机译：反式咖啡因类似物的合成及其对HIV-1整合酶和癌细胞系的生物活性。

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摘要

Forty caffeate analogues were synthesized via a convenient method starting from vanillin with moderate to good yields. The testing of biological activity of these compounds against HIV-1 integrase indicates that four compounds: bornyl caffeate, bornyl 2-nitrocaffeate, 5-nitrocaffeic acid and 5-nitrocaffeic acid phenethyl ester (5-nitroCAPE) possess a good HIV integrase inhibitory activity, IC(50) 19.9, 26.8, 25.0 and 13.5 microM , respectively. Twelve caffeate analogues were tested by MTT assay on growth of human hepatocellular carcinoma BEL-7404, human breast MCF-7 adenocarcinoma, human lung A549 adenocarcinoma and human gastric cancer BCG823 cell lines, respectively. And the best result is IC(50) 5.5 microM for CAPE against BEL-7404.

机译：通过方便的方法从香草醛开始以中等到良好的产率合成了40种咖啡酸盐类似物。这些化合物针对HIV-1整合酶的生物活性测试表明，四种化合物：咖啡酸冰片酯，2-硝基咖啡酸冰片酯，5-硝基咖啡酸和5-硝基咖啡酸苯乙酯（5-nitroCAPE）具有良好的HIV整合酶抑制活性， IC（50）分别为19.9、26.8、25.0和13.5 microM。通过MTT测定法分别测试了十二种咖啡酸盐类似物对人肝细胞癌BEL-7404，人乳腺MCF-7腺癌，人肺A549腺癌和人胃癌BCG823细胞系的生长。最好的结果是针对BEL-7404的CAPE的IC（50）5.5 microM。

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《Bioorganic and Medicinal Chemistry Letters》 |2008年第24期|共5页
作者
Xia CN; Li HB; Liu F; Hu WX;
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正文语种 eng
中图分类药学;生物化学;
关键词
Integrase; Human; HIV-1; Synthesis; Tumor cells; malignant; 整合酶;

机译：Integrase;Human;HIV-1;Synthesis;Tumor cells;malignant;整合酶;

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1. Synthesis of trans-caffeate analogues and their bioactivities against HIV-1 integrase and cancer cell lines. [J] . Xia CN, Li HB, Liu F, Bioorganic and Medicinal Chemistry Letters . 2008,第24期

机译：反式咖啡因类似物的合成及其对HIV-1整合酶和癌细胞系的生物活性。
2. Docking, Synthesis and Biological Evaluation of Novel Diketoquinoline Analogues as HIV-1 Integrase Inhibitor [J] . Kishore D. Deo, I.J. Singhvi, S.R. Patil Asian Journal of Chemistry: An International Quarterly Research Journal of Chemistry . 2019,第9期

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5. Design and synthesis of molecular probes to modulate cell membrane permeation: I. Design, synthesis, and biological evaluation of novel chicoric acid analogues as inhibitors of HIV-1 integrase. II. Design, synthesis, and biological evaluation of novel estradiol analogues targeting the membrane estrogen receptor. [D] . Charvat, Trevor Thomas. 2004

机译：设计和合成的分子探针，可调节细胞膜的渗透性：I.设计，合成和生物评价作为抗HIV-1整合酶抑制剂的新型菊苣酸类似物。二。针对膜雌激素受体的新型雌二醇类似物的设计，合成和生物学评估。
6. Vitamin D analogues up-regulate p21 and p27 during growth inhibition of pancreatic cancer cell lines. [O] . S. Kawa, T. Nikaido, Y. Aoki, 1997

机译：在胰腺癌细胞系生长抑制过程中维生素D类似物上调p21和p27。
7. Synthesis and HIV-1 Integrase Inhibition of Novel Bis- or Tetra-Coumarin Analogues [O] . Chih-Chia Chiang, Jean-François Mouscadet, Hou-Jen Tsai, 2007

机译：新型双或四香豆素类似物的合成和HIV-1整合酶抑制

Synthesis of trans-caffeate analogues and their bioactivities against HIV-1 integrase and cancer cell lines.

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