Sophoridine - CAS 6882-68-4

Sophoridine (Dihydro-5-episophocarpine), a natural anticancer drug, has been used in China for decades. A series of novel N-substituted Sophoridinic acid derivatives were synthesized and evaluated for their cytotoxicity with 1 as the lead. The structure-activity relationship indicated that introduction of an aliphatic acyl on the nitrogen atom might significantly enhance the anticancer activity. Among the compounds, 6b bearing bromoacetyl side-chain afforded a potential effect against four human tumor cell lines (liver, colon, breast, and lung) . The mechanism of action of 6b is to inhibit the activity of DNA topoisomerase I, followed by the S-phase arrest and then cause apoptotic cell death, similar to that of its parent 1.

Topoisomerase, Apoptosis

DNA Damage/DNA Repair, Apoptosis

6810

0.9928

C15H24N2O

248.36

O=C1N2[C@@]([C@@]3([C@@]4([C@@](C2)(CCCN4CCC3)[H])[H])[H])(CCC1)[H]

-20°C

Ice Packs

Natural Product