Discovery of novel dithiocarbamic acid ester HGWJ-11C with significant anticancer action

新型氨基二硫代甲酸酯类抗肿瘤化合物HGWJ-11C的发现(英文)

To find novel lead compound, seventy-four compound libraries were built through two rounds by a solution-phase CC on the basis of our developed method for the synthesis of dithiocarbamic acid ester. After evaluation for the antitumor activities of libraries, six compounds were selected to be synthesized and examined their antitumor activities. It was found that compound 13 （HGWJ-11 C） with novel structure exhibited significant antitumor activities and the scaffold of dithiocarbamic acid was very crucial for the antitumor activity. The compound 13 is worth studying deeply as a potent hit compound.

为发现新结构类型的抗肿瘤化合物,基于我们发现的氨基二硫代甲酸酯类化合物的合成新方法,利用液相组合化学技术,通过两轮共构建了74个化合物库,对从中筛选出的6个可能具有活性的化合物进行了合成及活性验证,发现结构新颖的化合物13(HGWJ-11C)具有明显抗肿瘤作用,其中的氨基二硫代甲酸骨架是产生活性的必需结构。化合物13值得作为一个苗头化合物进行深入研究。