Disclosed herein are novel bifunctional compounds and their uses for the treatment and/or prophylaxis of cancers. The bifunctional compound disclosed herein has the structure of formula (I),wherein, A is an optionally substituted 6-10 membered unsaturated carbon cycle； R1is an alkyl optionally substituted with halo, -OR, -OAc, -OSO2R, or -OCONHR, in which R is hydrogen, alkyl, cycloalkyl, or aryl； R2is hydrogen, alkyl,cycloalkyl, aryl or heteroaryl； R3is –NRARB, –NHPhRC, mono- or bis-saccharide(s) group, or an amino acid group, or -NRARBare taken together to form an optionally substituted aniline or cycloalkylamine selected from the group consisting of morpholine, pyrrolidine, piperidine, 1-substituted piperazine, 1,4’-bipiperidine, 4’-substituted 4,4’-bipiperidine； wherein the substituent on piperazine and 4,4’-bipiperidine is alky, -(CH2)nCONH(CH2)mNRARB, wherein n and m are independently an integral between 1 to 5, and RAand RBare independently H or C1-C6alkyl； and RCis hydrogen, halo, alkoxy, –CH2OH, –NHCORa, –NHC(O)ORa, or optionally substituted alkyl, alkenyl, alkynyl, herocyclyl, or aryl, and Rais C1-6alkyl or aryl； and the aryl or heteroaryl is optionally substituted with at least one substituent selected from the group consisting of C1-6alkyl, alkoxy, halo, cyano, nitro, -NH2, -NHRc, -N(Rc)2, cycloalkylamino, methylenedioxy or ethylenedioxy group, in which Rcis independently hydrogen or C1-10alkyl.本揭示內容是關於新穎的雙功化合物及其於治療及／或預防癌症之用途。本揭示內容雙功化合物具有式(I)之結構，其中， A是一有或無取代基之6–10員不飽和碳環； R1是一有或無鹵素、–OR、–OAc、–OSO2R或–OCONHR取代的烷基，其中R是氫、烷基、環烷基或芳基； R2是氫、烷基、環烷基、芳基或雜芳基； R3是–NRARB、–NHPhRC、單或雙醣基，或是一胺基酸基，或是–NRARB合併形成一有或無取代基之苯胺或環烷基胺，其係選自由嗎啉、吡咯啶、哌啶、1–經取代之哌嗪、1,4’–聯哌啶及4’–經取代之4,4’–聯哌啶所組成的群組；其中哌嗪及4,4’–聯哌啶的取代基是烷基、–(CH2)nCONH(CH2)mNRARB，其中n及m個別是一介於1至5的整數，且RA及RB個別是H或C1–C6烷基；以及 RC是氫、鹵素、烷氧基、–CH2OH、–NHCORa、–NHC(O)ORa，或是有或無取代基之烷基、烯基、炔基、雜環基或芳基，且Ra是C1–6烷基或芳基；以及 非必要地，該芳基或雜芳基具有至少一取代基，其中該至少一取代基係選自由C1–6烷基、烷氧基、鹵素、氰基、硝基、–NH2、–NHRc、–N(Rc)2、環烷胺基、亞甲二氧基及伸乙二氧基所組成的群組，其中Rc個別是氫或C1–10烷基。
