(PubMed) Ren X, Xu P, Zhang D, et al
Tumor targeting with novel Pyridyl 6-substituted Pyrrolo [2,3-d] pyrimidine Antifolates via cellular uptake by folate receptor and the proton-coupled folate transporter and inhibition of De novo purine nucleotide biosynthesis
For example, the spacer can be selected from the group consisting of -C1-C10 alkylene- , -C1-C10 heteroalkylene-, -C3-C8 carbocyclo-, -O-(Ci Cs alkyl)-, -arylene-, -C1-C10 alkylene-arylene-, -arylene-C-i-C-io alkylene-, -C1-C10 alkylene-(C3-Cs carbocyclo)-, -(C3- Cs carbocyclo)-Ci-Cio alkylene-, -C3-C8 heterocyclo-, -C1-C10 alkylene-(C3- Cs heterocyclo)-, -(C3-C8 heterocyclo)-Ci-Cio alkylene-, -C1-C10 alkylene-C(=O)-, -C1- C10 heteroalkylene-C(=O)-, -C3-C8 carbocyclo-C(=O)-, -O-(Ci-Cs alkyl)-C(=O)-, -arylene- C(=O)-, -C1-C10 alkylene-arylene-C(=O)-, -arylene-Ci-Cw alkylene-C(=O)-, -C1- C10 alkylene-(C3-C8carbocyclo)-C(=O)-, -(C3-C8 carbocyclo)-Ci-Cio alkylene-C(=O)-, - C3-C8 heterocyclo-C(=O)-, -C1-C10 alkylene-(C3-C8heterocyclo)-C(=O)-, -(C3- Cs heterocyclo)-Ci-Cio alkylene-C(=O)-, -C1-C10 alkylene-NH-, -C1-C10 heteroalkylene- NH-, -C3-C8 carbocyclo-NH-, -O-(Ci-Cs alkyl)-NH-, -arylene-NH-, -C1-C10 alkylene- arylene-NH-, -arylene-Ci-Cw alkylene-NH-, -C1-C10 alkylene-(C3-Cs carbocyclo)-NH-, - (C3-C8 carbocyclo)-Ci-Cio alkylene-NH-, -Cs-Csheterocyclo-NH-, -C1-C10 alkylene-(C3- Cs heterocyclo)-NH-, -(C3-C8 heterocyclo)-Ci-Cio alkylene-NH-, -Ci-Cwalkylene-S-, -C1- C10 heteroalkylene-S -, -Cs-Cscarbocyclo-S -, -O-(Ci-Cs alkyl)-)-S -, -arylene-S-, -C1-C10 alkylene-arylene-S-, -arylene-Ci-Cw alkylene-S-, -Ci-Cio alkylene-(C3-Cs carbocyclo)-S- , -(C3-C8 carbocyclo)-Ci-Cio alkylene-S-, -C3-C8 heterocyclo-S-, -C1-C10 alkylene-(C3- Cs heterocyclo)-S-, -(C3-C8 heterocyclo)-Ci-Cio alkylene-S-, -C1-C10 alkylene-O-C(=O)-, -C3-C8 carbocyclo-O-C(=O)-, -O-(Ci-Cs alkyl)-O-C(=O)-, -arylene-O-C(=O)-, -C1- C10 alkylene-arylene-O-C(=O)-, -arylene-Ci-Cw alkylene-O-C(=O)-, -C1-C10 alkylene- (C3-C8carbocyclo)-O-C(=O)-,-(C3-C8 carbocyclo)-Ci-Cio alkylene-O-C(=O)-, -C3- Cs heterocyclo-O-C(=O)-, -C1-C10 alkylene-(C3-C8heterocyclo)-O-C(=O)-, and -(C3- Cs heterocyclo)-Ci-Cio alkylene-O-C(=O)-
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