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...

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Bibliographische Detailangaben
Hauptverfasser:	TERCEL, Moana, LEE, Ho Huat
Format:	Patent
Sprache:	eng
Schlagworte:	CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
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Beschreibung
Zusammenfassung:	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.