Conformationally defined retinoic acid analogues.: 5.: Large-scale synthesis and mammary cancer chemopreventive activity for (2E,4E,6Z,8E)-8(3',4'-dihydro-1'(2'H)-naphthalen-1'-ylidene)-3,7-dimethyl-2,4,6-octatrienoic acid (9cUAB30)
Conformationally defined retinoic acid analogues.: 5.: Large-scale synthesis and mammary cancer chemopreventive activity for (2E,4E,6Z,8E)-8(3',4'-dihydro-1'(2'H)-naphthalen-1'-ylidene)-3,7-dimethyl-2,4,6-octatrienoic acid (9cUAB30)
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DOI：
10.1021/jm030095q
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发表时间：
2003-08-14
影响因子：
7.3
通讯作者：
Muccio, DD
中科院分区：
文献类型：
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作者：
Atigadda, VR;Vines, KK;Muccio, DD
激活核维甲酸X受体（RXR）的维甲酸显示出化学预防乳腺癌的潜力。我们先前报道了9 cUAB 30（1）是一种RXR选择性维甲酸。为了探索其体内化学预防活性，需要数克量的1。在这里，我们描述了一种改进的合成，产生高达100克的1。我们进一步证明，1是非常有效的预防N-甲基-N-亚硝基脲诱导的大鼠乳腺癌没有毒性的迹象。
Retinoids that activate the nuclear retinoid X receptors (RXRs) display potential for chemo-prevention of breast cancer. We previously reported that 9cUAB30 (1) is an RXR-selective retinoid. To explore its in vivo chemopreventive activity, multigram quantities of 1 were needed. Here, we describe a modified synthesis that yields up to 100 g of 1. We further demonstrate that 1 is very effective in the prevention of N-methyl-N-nitrosourea induced mammary cancers in rats without signs of toxicity.