KN-62 analogues as potent differentiating agents of HL-60 cells.

Abstract:

:KN-62, an inhibitor of the calmodulin-dependent protein kinases (CaMKs), enhances the terminal differentiation of retinoic acid sensitive human myeloid leukemia cell lines. In an effort to identify additional CaMK inhibitors that exhibit more potent activity in triggering leukemia cell differentiation, we synthesized 45 analogues of KN-62 and determined their ability to induce HL-60 cell differentiation. Sixteen of these novel analogues exhibited significant differentiation-inducing activity, and one analogue, AS-004, was five times more potent than KN-62 in inhibiting proliferation and inducing differentiation of HL-60 cells. Such KN-62 analogues and/or related compounds may prove useful in treating promyelocytic leukemia.

journal_name

Leuk Res

journal_title

Leukemia research

authors

Schuler AD,Si J,Mueller L,Simon JA,Collins SJ

doi

10.1016/j.leukres.2006.07.022

subject

Has Abstract

pub_date

2007-05-01 00:00:00

pages

683-9

issue

5

eissn

0145-2126

issn

1873-5835

pii

S0145-2126(06)00282-7

journal_volume

31

pub_type

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