The invention provides a protected anti-neoplastic agent of the formula Hyp-N, wherein N is an anti-neoplastic agent and a protectable hydroxyl group of the anti-neoplastic is substituted with Hyp; Hyp is a moiety having the formula: wherein R 2 is hydrogen; R 3 is hydrogen or C 1 -C 6 alkyl; R 1 is C 1 -C 6 alkyl or C 1 -C 6 alkoxy, optionally substituted with one or more heteroatom-containing groups; and R 4 is hydrogen, C 1 -C 6 alkyl, or C 1 -C 6 alkoxy, optionally substituted with one or more heteroatom-containing groups.저산소증 활성화된 프로드러그가 단독으로 또는 하나 이상의 항신생물제와 병용 투여되는 경우에 암을 치료하는 데 사용될 수 있다.