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Synthesis of NSC 106084 and NSC 14778 and evaluation of their DNMT inhibitory activity.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2019-01-22 , DOI: 10.1016/j.bmcl.2019.01.022 Maxime Leroy 1 , Léa Mélin 1 , Steven R LaPlante 2 , José L Medina-Franco 3 , Alexandre Gagnon 1
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2019-01-22 , DOI: 10.1016/j.bmcl.2019.01.022 Maxime Leroy 1 , Léa Mélin 1 , Steven R LaPlante 2 , José L Medina-Franco 3 , Alexandre Gagnon 1
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DNA methylation is an epigenetic modification that is performed by DNA methyltransferases (DNMTs) and that leads to the transfer of a methyl group from S-adenosylmethionine (SAM) to the C5 position of cytosine. This transformation results in hypermethylation and silencing of genes such as tumor suppressor genes. Aberrant DNA methylation has been associated with the development of many diseases, including cancer. Inhibition of DNMTs promotes the demethylation and reactivation of epigenetically silenced genes. NSC 106084 and 14778 have been reported to inhibit DNMTs in the micromolar range. We report herein the synthesis of NSC 106084 and 14778 and the evaluation of their DNMT inhibitory activity. Our results indicate that while commercial NSC 14778 is moderately active against DNMT1, 3A/3L and 3B/3L, resynthesized NSC 14778 is inactive under our assay conditions. Resynthesized 106084 was also found to be inactive.
中文翻译：
NSC 106084和NSC 14778的合成及其DNMT抑制活性的评估。
DNA甲基化是一种表观遗传修饰，由DNA甲基转移酶（DNMT）进行，导致甲基从S-腺苷甲硫氨酸（SAM）转移到胞嘧啶的C5位置。该转化导致诸如肿瘤抑制基因的基因的超甲基化和沉默。DNA甲基化异常与许多疾病的发展有关，包括癌症。DNMT的抑制促进表观遗传沉默基因的去甲基化和再激活。据报道，NSC 106084和14778可以在微摩尔范围内抑制DNMT。我们在此报告了NSC 106084和14778的合成及其对DNMT抑制活性的评估。我们的结果表明，虽然商用NSC 14778对DNMT1、3A / 3L和3B / 3L具有中等活性，重新合成的NSC 14778在我们的测定条件下是无活性的。还发现重新合成的106084不活跃。
更新日期：2019-01-22
中文翻译：
NSC 106084和NSC 14778的合成及其DNMT抑制活性的评估。
DNA甲基化是一种表观遗传修饰，由DNA甲基转移酶（DNMT）进行，导致甲基从S-腺苷甲硫氨酸（SAM）转移到胞嘧啶的C5位置。该转化导致诸如肿瘤抑制基因的基因的超甲基化和沉默。DNA甲基化异常与许多疾病的发展有关，包括癌症。DNMT的抑制促进表观遗传沉默基因的去甲基化和再激活。据报道，NSC 106084和14778可以在微摩尔范围内抑制DNMT。我们在此报告了NSC 106084和14778的合成及其对DNMT抑制活性的评估。我们的结果表明，虽然商用NSC 14778对DNMT1、3A / 3L和3B / 3L具有中等活性，重新合成的NSC 14778在我们的测定条件下是无活性的。还发现重新合成的106084不活跃。
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