MODIFIED CYTOTOXINS AND THEIR THERAPEUTIC USE

摘要

The present disclosure generally provides compounds useful for treating cancer. In some aspects, the disclosure provides small-molecule cytotoxins that are chemically modified to include one or more moieties that include hydrophobic portions. In some embodiments, the disclosure provides small-molecule cytotoxins that are chemically modified with fatty acid-containing moieties. In some aspects, the disclosure provides compositions, such as pharmaceutical compositions, that include such modified small-molecule cytotoxins and a protein. In some embodiments, the protein is albumin or an albumin mimetic. Further, the disclosure provides various uses of these compounds and compositions.

主权项

1. A compound of formula (I)
A1-X1—X2-A2   (I)wherein:
A1 is a hydrophilic group; A2 is a cytotoxic drug moiety, which has a molecular weight of no more than 1600 Da; X1 is —(CH2)12—, —(CH2)14—, —(CH2)16—, —(CH2)18—, —(CH2)20—, or —(CH2)22—; and X2 is a direct bond, or an organic group.