Duocarmycin analogues

The invention relates to 2-methylbenzoxazole compounds of formula I which are analogues of the DNA alkylating subunit of the duocarmycins. Compounds of formula I can be used in the synthesis of DNA alkylating agents and antibody-drug conjugates and related compounds. The 2-methylbenzoxaxole unit of formula I has advantageous properties in combining high cytotoxicity, low lipophilicity, and unusual aqueous stability, all of which are desirable for application as payloads in efficacious antibody-drug conjugates. 本发明涉及式I的2-甲基苯并噁唑化合物，其为倍癌霉素的DNA烷基化亚单位的类似物。式I化合物可用于合成DNA烷基化剂和抗体-药物缀合物以及相关化合物。式I的2-甲基苯并噁唑单元在结合高细胞毒性、低亲脂性和异常的水稳定性方面具有有利的性质，所有这些性质对于在有效的抗体-药物缀合物中作为有效负荷的应用是合乎需要的。