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ALK Inhibitors of Bis-Ortho-Alkoxy-Para-Piperazinesubstituted-Pyrimidines and -Triazines for Cancer Treatment

ALK Inhibitors of Bis-Ortho-Alkoxy-Para-Piperazinesubstituted-Pyrimidines and -Triazines for Cancer Treatment

Hyeon Ji Lee, Muhammad Latif, Hyeonjeong Choe, Imran Ali, Heung Kyoung Lee, Eun Hye Yang, Jeong In Yun, Chong Hak Chae, Jae-Kyung Jung, Hyoung Rae Kim, Chong Ock Lee, Chi Hoon Park, Kwangho Lee

Arch Pharm Res. 2014;37(9):1130-8.

PMID: 24446111

Abstract:

Syntheses of various bis-ortho-alkoxy-para-piperazineanilino-pyrimidines and -triazines of KRCA-0008 analogs are described and their structure-activity-relationship to anaplastic lymphoma kinase (ALK) is discussed. 5-trifluoromethyl-2,4-pyrimidine analog (2) seems to be most potent in both biochemical and cellular assay in this study, however it shows inferior mice xenograft activity to Crizotinib presumably due to its sub-optimal PK parameters. 4,6-disubstituted pyrimidine and 2,4-disubstituted triazine derivatives of KRCA-0008 are less potent or inactive to ALK wt., and this observation is explained with their molecular modeling compared to KRCA-0008.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1472795202	KRCA-0008		1472795-20-2	Price

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