Provided are phenylbutyryl curcumin derivatives, their preparation methods, pharmaceutical compositions containing said derivatives and uses thereof for preparing anti-tumor drugs. Said curcumin derivatives are specifically 4-[bis(2-chloroethyl)amino]phenylbutyryl curcumin and 4,4'-bis[bis(2-chloroethyl)amino]phenylbutyryl curcumin, and their pharmaceutically acceptable salts. The curcumin derivatives are effective on inhibiting various animal tumor cell transplantation models in vivo, and do not have serious toxicity in mouse.
