1224708-65-9Relevant academic research and scientific papers
Novel bis-ortho-alkoxy-para-piperazinesubstituted-2,4-dianilinopyrimidines (KRCA-0008) as potent and selective ALK inhibitors for anticancer treatment
Park, Chi Hoon,Choe, Hyeonjeong,Jang, In-Young,Kwon, So Yeong,Latif, Muhammad,Lee, Heung Kyoung,Lee, Hyeon Ji,Yang, Eun Hye,Yun, Jeong In,Chae, Chong Hak,Cho, Sung Yun,Choi, Sang Un,Ha, Jae Du,Jung, Heejung,Kim, Hyoung Rae,Kim, Pilho,Lee, Chong Ock,Yun, Chang-Soo,Lee, Kwangho
, p. 6192 - 6196 (2013)
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.
N2,N4-BIS(4-(PIPERAZINE-1-YL)PHENYL)PIRIMIDINE-2,4-DIAMINE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, AND COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT FOR PREVENTING OR TREATING CANCER
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, (2015/06/10)
Disclosed herein are a new N2,N4-bis(4-(piperazin-1-yl)phenyl)pyrimidin-2,4-diamine derivative or a pharmaceutically acceptable salt thereof and a pharmaceutical composition for the prevention or treatment of cancers containing the same as an active ingredient. The compound of the present invention has excellent inhibitory effects against the activities of anaplastic lymphoma kinase (ALK) and activated cdc42-associated kinase (ACK1) and thus can improve the therapeutic effects on the treatment of cancer cells having anaplastic lymphoma kinase fusion proteins such as EML4-ALK and NPM-ALK, and also effectively prevent the recurrence of cancers thus being useful as a pharmaceutical composition for the prevention and treatment of cancers.
N2,N4-BIS(4-(PIPERAZINE-1-YL)PHENYL)PIRIMIDINE-2,4-DIAMINE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, AND COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT FOR PREVENTING OR TREATING CANCER
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, (2015/07/02)
The present invention relates to a N2,N4-bis(4-(piperazine-1-yl)phenyl)pirimidine-2,4-diamine derivative or a pharmaceutically acceptable salt thereof, and to a composition containing same as an active ingredient for preventing or treating cancer. Since the compound according to the present invention has good effects in inhibiting the activities of anaplastic lymphoma kinase (ALK) and activated Cdc42-associated kinase (ACK1), the compound can have improved therapeutic effects against cancer cells having ALK fusion proteins such as EML4-ALK and NPM-ALK and is expected to be effective in preventing the recurrence of cancer. Therefore, the compound can be effectively used as a composition for preventing or treating cancer.
