Enediyne compounds, conjugates thereof, and uses and methods therefor

A method of treating a cancer in a subject suffering from such cancer, comprising administering to the subject a therapeutically effective amount of a compound having a structure represented by formula (I), or a conjugate thereof with a targeting moiety:

• wherein
• R0 is NHR1a, NHC(═O)OR1b, NHC(═O)NHR1b, OC(═O)NHR1b, (CH2)1-4NHR1a, F, Cl, Br, OR1a, or SR1b;
• R1a is H, C1-C6 alkyl, (CH2)nNH2, C(═O)(CH2)nNH2, C(═O)CHR8NH2, or C(═O)R9NH2;
• R1b is H, C1-C6 alkyl, (CH2)nNH2,
• R2 is H, R10, C(═O)R10, or C(═O)OR10;
• R3 is H or unsubstituted or substituted C1-C6 alkyl;
• R4 is OH, SH, NH2, OR10, SR10, NHR10, N(R10)2, NHC(═O)OR10, OC(═O)NHR1b, OC(═O)R10, SC(═O)R10, or NHC(═O)R10;
• R5 is OH, SH, NH2, OR10, SR10, NHR10, N(R10)2, NHC(═O)OR10, OC(═O)NHR1b, OC(═O)R10, SC(═O)R10, or NHC(═O)R10;
• R6 is H or unsubstituted or substituted C1-C6 alkyl;
• or R5 and R6 combine to form ═O;
• R7 is OH, SH, NH2, OR10, SR10, NHR10, N(R10)2, NHC(═O)OR10, OC(═O)NHR1b, OC(═O)R10, SC(═O)R10, or NHC(═O)R10;
• R8 is the side chain residue of an α-amino acid selected from the group consisting of alanine, arginine, asparagine, aspartic acid, γ-carboxyglutamic acid, citrulline, cysteine, glutamic acid, glutamine, glycine, histidine, isoleucine, leucine, lysine, methionine, norleucine, norvaline, ornithine, phenylalanine, serine, threonine, tryptophan, tyrosine, and valine;
• R9 is unsubstituted or substituted arylene, unsubstituted or substituted heteroarylene, unsubstituted or substituted alkylarylene, unsubstituted or substituted cycloalkylene or unsubstituted or substituted heterocycloalkylene;
• each R10 is independently unsubstituted or substituted C1-C6 alkyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted heterocycloalkyl, unsubstituted or substituted arylalkyl, unsubstituted or substituted aryl;
• or unsubstituted or substituted heteroaryl;
• and
• n is 2, 3, 4, 5, or 6;
• or a pharmaceutically acceptable salt thereof.