| 摘要 |
The invention provides linker compounds containing a disulfide group, and maytansin-derived cytotoxic compounds that are useful for forming a CBA-drug conjugates, and conjugates so formed. Such conjugates and/or cytotoxic compounds may be effective for treating a range of diseases, such as cancer, with a relatively high activity at a relatively low, non-toxic dose. |
| 主权项 |
1. A conjugate represented by the following formula, or a pharmaceutically acceptable salt thereof: wherein:
CBA is a cell binding agent;DM is a drug moiety represented by the following formula: R, R′, and R″, for each occurrence, are independently H or an optionally substituted alkyl;
Y is —(CR3R4)—CR1R2—;R1-R4, for each occurrence, are independently H, an optionally substituted alkyl, an optionally substituted alkenyl, an optionally substituted cycloalkyl, an optionally substituted heterocyclyl, an optionally substituted aryl, or an optionally substituted heteroaryl;n is an integer between 0 and 15; andw is an integer between 1 and 20.provided that CBA does not comprise a modified lysine residue carrying a free thiol (—SH) group. |
