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Synthesis of fluorescent analogues of the anticancer natural products 4-hydroxyphenylmethylene hydantoin and δ-tocotrienol

机译:抗癌天然产物4-羟苯基亚甲基乙内酰脲和δ-生育三烯酚的荧光类似物的合成

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摘要

4-Hydroxyphenylmethylene hydantoin (PMH, 1), isolated from the Red Sea sponge Hemimycale arabica, and δ-tocotrienol (3), isolated from the tocotrienol-rich fraction of palm oil, are important antimetastatic and antiproliferative natural products that proved effective against metastatic prostate and breast cancers, respectively. New fluorescent derivatives of PMH (2) and δ-tocotrienol (4) were synthesized by Steglich esterification. Both 2 and 4 retained good anti-migratory and antiproliferative activities, respectively. Fluorescent analogues 2 and 4 can be used for the identification of molecular targets of 1 and 3 in tumor cell cultures.
机译:从红海海绵Hemimycale arabica中分离出来的4-羟基苯基亚甲基乙内酰脲(PMH,1)和从棕榈油中富含生育三烯酚的馏分中分离出的δ-生育三烯酚(3)是重要的抗转移和抗增殖天然产物,已证明对转移具有有效的抑制作用前列腺癌和乳腺癌。通过Steglich酯化反应合成了新的PMH(2)和δ-生育三烯酚(4)的荧光衍生物。 2和4分别保留了良好的抗迁移和抗增殖活性。荧光类似物2和4可用于鉴定肿瘤细胞培养物中1和3的分子靶标。

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