FLUORESCENT CELL CYCLE PROBE HAVING M-PHASE SPECIFICITY

摘要

The present invention is directed to a novel family of fluorophores based on the BODIPY scaffold, and methods for their synthesis. The BODIPY-based fluorophores disclosed herein are used for the selective visualization of cells that exist in the M-phase of the cell cycle. The present invention further relates to methods for the image-based monitoring of mitotic progression in live cells.

主权项

1. A compound having the structure of Formula (I) or a pharmaceutically acceptable salt thereof:wherein:
R1 is (C6-C10)aryl or (C3-C12)heteroaryl, optionally substituted at any position with one or more substituents, each substituent independently selected from (C1-C10)alkyl, —O(C1-C6)alkyl, (C2-C6)alkenyl, (C6-C10)aryl, —O(C6-C10)aryl, —S(C1-C10)alkyl, —O(benzyl), (C3-C8)heteroaryl, halo, hydroxyl, NR3R4, nitro or —O(C2-C6)alkenyl; further wherein each —O(C1-C6)alkyl, (C2-C6)alkenyl, —O(C6-C10)aryl, —O(benzyl) or (C3-C8)heteroaryl is optionally substituted at any position with one or more substituents, each independently selected from halo, (C6-C10)aryl, (C1-C10)alkyl or —O(C1-C6)alkyl; R2 is (C1-C6)alkyl or (C3-C8)cycloalkyl, optionally and independently substituted with one or more substituents selected from NR5R6, hydroxyl, halo or —O(C1-C6)alkyl; and R3, R4, R5, and R6, if present, are each independently selected from H, (C1-C6)alkyl, (C6-C10)aryl, (C1-C6)hydroxyalkyl, or are taken together to form a (C3-C7)heterocycle.