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Synthesis of new dihydroberberine and tetrahydroberberine analogues and evaluation of their antiproliferative activity on NCI-H1975 cells.
Beilstein Journal of Organic Chemistry ( IF 2.2 ) Pub Date : 2020-07-06 , DOI: 10.3762/bjoc.16.133
Giacomo Mari 1 , Lucia De Crescentini 1 , Serena Benedetti 2 , Francesco Palma 2 , Stefania Santeusanio 1 , Fabio Mantellini 1
Affiliation  

Dihydroberberine (DHBER), the partially reduced form of the alkaloid berberine (BER), is known to exhibit important biological activities. Despite this fact, there have been only few studies that concern the biological properties of functionalized DHBER. Attracted by the potentiality of this latter compound, we have realized the preparation of new arylhydrazono-functionalized DHBERs, starting from BER and some α-bromohydrazones. On the other hand, also the fully reduced form of BER, namely tetrahydroberberine (THBER), and its derivatives have proven to present different biological activities. Therefore, the obtained arylhydrazono-functionalized DHBERs were reduced to the corresponding arylhydrazono-THBERs. The antiproliferative activity of both arylhydrazono-DHBERs and -THBERs has been evaluated on NCI-H1975 lung cancer cells.

中文翻译:

新型二氢小檗碱和四氢小檗碱类似物的合成及其对NCI-H1975细胞的抗增殖活性评估。

二氢小檗碱 (DHBER) 是生物碱小檗碱 (BER) 的部分还原形式,已知具有重要的生物活性。尽管如此,有关功能化 DHBER 生物学特性的研究却很少。受到后一种化合物潜力的吸引,我们以 BER 和一些 α-溴腙为原料,实现了新型芳基腙官能化 DHBER 的制备。另一方面,BER 的完全还原形式,即四氢小檗碱 (THBER) 及其衍生物也已被证明具有不同的生物活性。因此,获得的芳基腙官能化的DHBER被还原为相应的芳基腙-THBER。芳基肼基-DHBER 和-THBER 的抗增殖活性已在 NCI-H1975 肺癌细胞上进行了评估。
更新日期:2020-07-06
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