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US 2026/0216352 A1Published application
Directed biosynthesis of modified anthraquinone-fused enediynes as potential cancer therapeutics
AssigneeThe Johns Hopkins University
InventorsCraig A. TOWNSEND, Paramita PAL, Jamie ALLEY
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Abstract
Analogues of dynemicin, methods of their preparation, and their use for treating cancer are disclosed.
Claims38
A compound of formula (I):
- wherein:
- R1 is selected from H, hydroxyl, and —O—(C═O)—CH3;
- R2 and R3 are each independently selected from H, hydroxyl, C1-C4 alkyl, C1-C4 alkoxyl, halogen, carbonyl, carboxyl, acetyl, cyano, mercapto, nitro, —O—(C═O)—CH3, and —(CH2)n—NR6R7, wherein n is an integer selected from 0, 1, 2, 3, and 4, R6 and R7 are each independently selected from H, C1-C4 alkyl, and a protecting group;
- R5 is hydroxyl or —O—(C═O)—CH3;
- provided that if R1, R4, and R5 are each hydroxyl, then R2 and R3 cannot both be H;
- and;
- stereoisomers and pharmaceutically acceptable salts thereof.
4 more elements
(canceled)
(canceled)
-11. (canceled)
A compound of formula (II):
- wherein:
- Y is selected from halogen, hydroxyl, methoxyl, and —O—S(═O)2—CF3 (—OTf);
- and
- R3 is selected from halogen, C1-C4 alkyl, —C(═O)—CH3, —NH—C(═O)—CH3, cyano, and —(CH2)n—NR6R7, wherein n is an integer selected from 0, 1, 2, 3, and 4, R6 and R7 are each independently selected from H, C1-C4 alkyl, and a protecting group.
1 more element
A method for generating dynemicin or an analogue thereof, the method comprising:
- culturing a plurality of mutant Micromonospora lacking ORF15 in growth media supplemented with an iodoanthracene for a period of time and under conditions sufficient to process the iodoanthracene;
- and
- purifying the dynemicin or analogue thereof.
Dependencies are inferred from the claim text.