Synthesis of new dihydroberberine and tetrahydroberberine analogues and evaluation of their antiproliferative activity on NCI-H1975 cells.

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 aryl hydrazono-functionalized DHBERs, starting from BER and some -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 aryl hydrazono-functionalized DHBERs were reduced to the corresponding aryl hydrazono-THBERs. The antiproliferative activity of both aryl hydrazono-DHBERs and -THBERs has been evaluated on NCI-H1975 lung cancer cells.