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Novel bis-ortho-alkoxy-para-piperazinesubstituted-2,4-dianilinopyrimidines (KRCA-0008) as potent and selective ALK inhibitors for anticancer treatment.

Abstract：

:The synthesis of bis-ortho-alkoxy-para-piperazinesubstituted-2,4-dianilinopyrimidines is described and their structure-activity-relationship to anaplastic lymphoma kinase (ALK) is presented. KRCA-0008 is selective and potent to ALK and Ack1, and displays drug-like properties without hERG liability. KRCA-0008 demonstrates in vivo efficacy comparable to Crizotinib in xenograft mice model.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Park CH,Choe H,Jang IY,Kwon SY,Latif M,Lee HK,Lee HJ,Yang EH,Yun JI,Chae CH,Cho SY,Choi SU,Ha JD,Jung H,Kim HR,Kim P,Lee CO,Yun CS,Lee K

doi

10.1016/j.bmcl.2013.08.090

subject

Has Abstract

pub_date

2013-11-15 00:00:00

pages

6192-6

issue

22

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(13)01039-1

journal_volume

23

pub_type

杂志文章

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