Antiproliferative compounds, conjugates thereof, methods therefor, and uses thereof
View Patent ↗Antiproliferative compounds having a structure represented by formula (II), where n, R 1 , R 2 , R 3 , R 4 , and R 5 are as defined herein, can be used to treat tumors, optionally when conjugated to a ligand such as an antibody:
1. A compound having a structure according to formula (VIII-a)
wherein R 7 is H or an amine protecting group and R 8 is H, C 1 -C 10 alkyl, C 2 -C 10 alkenyl, C 2 -C 10 alkynyl, aryl, cycloaliphatic, alkylcycloaliphatic, arylalkyl, or alkylaryl.
2. A compound according to claim 1 , wherein R 8 is H or C 1 -C 5 alkyl.
3. A compound according to claim 2 , wherein R 8 is Me.
4. A compound according to claim 1 , wherein R 7 is H, Boc (t-butoxycarbonyl), Troc (2,2,2-trichloroethoxy carbonyl), Bpoc (1-methyl-1-(4-biphenyl)ethoxycarbonyl), Cbz (benzyloxy carbonyl), Aloc (allyloxycarbonyl), methyl amine, or Fmoc (9-fluorenylmethoxycarbonyl).
5. A compound according to claim 4 , wherein R 8 is H or C 1 -C 5 alkyl.
6. A compound according to claim 5 , wherein R 8 is Me.
7. A compound according to claim 1 , having a structure represented by the formula:
8. A compound according to claim 1 , having a structure represented by the formula:
9. A compound according to claim 1 , having a structure represented by the formula:
10. A compound according to claim 1 , having a structure represented by the formula: