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Twenty-two cephalotaxine-type and ten homoerythrina-type alkaloids, including seven previously undescribed ones, were isolated from the twigs and leaves and the seed kernels of
Cephalotaxus fortunei
. Their structures were established by spectroscopic analysis, single crystal X-ray diffraction, and ECD calculation methods. Cephalofortunine A β-
N
-oxide (1) is the first nitrogen-oxidized homoerythrina-type alkaloid. The isolated compounds were evaluated for their
in vitro
antiproliferative effects against two human leukemia cell lines (THP-1 and K562). All compounds showed different levels of antiproliferation in THP-1 and K562 cells with GI
50
values of 0.24–29.55 μM. Hainanensine (31) was the most active against two cancer cell lines with GI
50
values of 0.24 ± 0.07, and 0.29 ± 0.01 μM, respectively.