Abstract: The disclosure relates to the field of medicinal chemistry. Disclosed are a 14-chloro-?-elemene nitric oxide donor derivative and a preparation method and use thereof in the preparation of anti-tumor drugs. The 14-chloro-?-elemene nitric oxide donor derivative has a general formula shown in formula (I): in formula (I): R1 represents a linear or cyclic alcohol amine structure containing nitrogen and oxygen atoms; and each of R2 and R3 is independently selected from the group consisting of C1-10 alkyl, C3-12 cycloalkyl, C6-12 aryl, 5- to 10-membered cyclic heteroaryl, C2-10 alkenyl, C2-10 alkynyl, and C2-10 alkoxy.