Six new compounds including three lignanoids: reevesiacoumarin (1), reevesic acid (2), and reevesilignan (3), and three terpenoids: reevesiterpenol A (4), reevesiterpenol B (5), and 3 alpha, 27-di-O-trans-caffeoylbetulinic acid (6), along with 40 known compounds were isolated from the root and stem of Reevesia formosana (Sterculiaceae). The structures of 1-6 were determined by spectroscopic techniques. Bioassays for the cytotoxicities of MCF-7, NCI-H460, and HepG2 cancer cell lines led to finding three cardenolides: strophanthojavoside (31) and ascleposide (32) with IC50 < 1 mu M and strophalloside (33) displayed selective cytotoxicity to NCI-H460 with IC50 0.62 +/- 0.06 mu M as well. 3 alpha, 27-Di-O-trans-caffeoylbetulinic acid (6) and secoisolariciresinol (13) also showed weak but selective cytotoxicity to NCI-H460 and HepG2 cancer cell lines, respectively.