Design, synthesis and optimization of Apcin analogues as Cdc20 inhibitors for triple-negative breast cancer therapy.

Cell division cycle 20 homologue (Cdc20) is an essential mitotic regulator whose overexpression is closely associated with tumorigenesis and poor prognosis in triple-negative breast cancer (TNBC). Targeting Cdc20 has therefore emerged as a promising therapeutic avenue for this aggressive malignancy. In the present study, a receptor-based drug design approach was employed to optimize Apcin analogues as Cdc20 inhibitors.

Serratane triterpenoids from Lycopodium complanatum and their anti-cancer and anti-inflammatory activities.

Phytochemical investigation of the ethyl acetate fraction of Lycopodium complanatum led to eight new serratane triterpenoids (lycomplanatums A-H, 1-8), along with five known analogues (9-13). Their structures were elucidated by extensive spectroscopic methods, including 1D/2D NMR, HRESIMS, and DFT GIAO C NMR calculation. Among them, compounds 2 and 13 showed moderate antiproliferative effects against seven human cancer cell lines, especially for MCF-7 with IC values of 13.