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Structure-Activity Relationship Study of Rakicidins: Overcoming Chronic Myeloid Leukemia Resistance to Imatinib with 4-Methylester-Rakicidin A.

Abstract：

:Natural product rakicidin A induces cell death in TKI-resistant chronic myelogenous leukemia (CML) cells. Therefore, 14 rakicidin A analogues were synthesized via a highly efficient combinatorial strategy and were evaluated against CML cell lines. The conjugated diene moiety was found to be crucial for the anti-CML activity of rakicidin A, and the changes in the configuration(s) at C-2, C-3, C-14, C-15, and C-16 resulted in lower levels of anti-CML activity. The most promising compound was 4-methylester rakicidin A (1a). Compared with rakicidin A, 1a exhibited 2.8-fold greater potency against the imatinib-resistant cell line K562/G(+) and approximately 100-fold enhanced potency compared with that of imatinib. Furthermore, compound 1a demonstrated a significantly lower resistance index against Ba/F3 cells expressing BCR-ABL(T315I) than bosutinib, dasatinib, nilotinib, and ponatinib, while 1a exhibited less effect on normal hematopoietic cells. Preliminary results indicated that 1a down-regulated caspase-3 and PARP, which contributes to its K562 cell inhibitory activity.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Sang F,Ding Y,Wang J,Sun B,Sun J,Geng Y,Zhang Z,Ding K,Wu LL,Liu JW,Bai C,Yang G,Zhang Q,Li LY,Chen Y

doi

10.1021/acs.jmedchem.5b01841

subject

Has Abstract

pub_date

2016-02-11 00:00:00

pages

1184-96

issue

3

eissn

0022-2623

issn

1520-4804

journal_volume

59

pub_type

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