Pentapeptide compounds and uses related thereto
View Patent ↗Pentapeptide compounds are disclosed. The compounds have biological activity, e.g., cytotoxicity. Prodrugs having targeting groups and pentapeptide moieities, as well as precursors thereof are also disclosed. For example, precursors having a reactive linker that can serve as a reaction site for joining to a targeting agent, e.g., an antibody, as disclosed.
1. A compound of the formula
and pharmaceutically acceptable salts and solvates thereof
wherein, independently at each location:
R 2 is selected from hydrogen and lower alkyl;
R 3 is lower alkyl;
R 4 is selected from lower alkyl, aryl, and —CH 2 —C 5-7 carbocycle when R 5 is selected from H and methyl, or R 4 and R 5 together form a carbocycle of the partial formula —(CR a R b ) n — wherein R a and R b are independently selected from hydrogen and lower alkyl and n is selected from 2, 3, 4, 5 and 6;
R 6 is selected from hydrogen and lower alkyl;
R 7 is sec-butyl or iso-butyl;
R 8 is selected from hydrogen and lower alkyl;
R 11 is selected from hydrogen and lower alkyl; and
R 18 is selected from hydrogen, a hydroxyl protecting group, and a direct bond where OR 18 represents ═O.
2. The compound of claim 1 of the formula
and pharmaceutically acceptable salts and solvates thereof.