1865-83-4Relevant articles and documents
Synthesis and photocleavage of a new polymerizable [2+2] hetero dimer for phototriggered drug delivery
Liese, Julia,Hampp, Norbert A.
, p. 228 - 234 (2011)
7-Hydroxy-1,1-dimethylnaphtalenone is introduced as a versatile photocleavable linker system for drug attachment to polymer materials with significantly improved two-photon-absorption efficiency. The synthesis of TBDMS-protected 7-hydroxy-1,1-dimethylnaphtalenone monomer is described, which is the release group attached to the polymer moiety. The cytotoxic 5-fluoro-1-heptanoyluracil was photochemically attached via [2+2] cycloaddition to this release group. The linker-drug conjugate was photochemically polymerized into a HEMA/MMA copolymer. Photo-triggered drug release from the polymer via single-photon-absorption as well as two-photon-absorption in solution were carried out. The detachment of 5-FU from the polymer and its release from the polymer were monitored in the polymer as well as in the aqueous medium and multidose drug release was successfully demonstrated.
4-(2-AMINO-TETRAHYDRONAPHTHALENYL)PYRIMIDINE DERIVATIVE, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING CANCER, CONTAINING SAME AS ACTIVE INGREDIENT
-
Paragraph 0170; 0171; 0172, (2018/04/26)
The present invention relates to a 4-(2-amino-tetrahydronaphthaleneyl)pyrimidine derivative, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of cancer comprising the same as an active ingredient. The 4-(2-amino-tetrahydronaphthaleneyl)pyrimidine derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention is very effective in suppressing anaplastic lymphoma kinase (ALK) activity and as a result it can improve the effectiveness of treatment on cancer cells having anaplastic lymphoma kinase (ALK) fusion proteins such as EML4-ALK and NPM-ALK, so that it can be effectively used as a pharmaceutical composition for preventing or treating cancer.
Novel 2,4-diaminopyrimidines bearing tetrahydronaphthalenyl moiety against anaplastic lymphoma kinase (ALK): Synthesis, in vitro, ex vivo, and in vivo efficacy studies
Song, Dawn,Lee, Minji,Park, Chi Hoon,Ahn, Sunjoo,Yun, Chang Soo,Lee, Chong Ock,Kim, Hyoung Rae,Hwang, Jong Yeon
supporting information, p. 1720 - 1725 (2016/07/27)
A series of novel 2,4-diaminopyrimidines bearing tetrahydronaphthalenyl moiety were synthesized and evaluated for their anti-anaplastic lymphoma kinase (ALK) activities using enzymatic and cell-based assays. Among the compounds synthesized, compound 17b showed promising pharmacological results in in vitro, ex vivo, and pharmacokinetic studies. An in vivo efficacy study with compound 17b demonstrated highly potent inhibitory activity in H3122 tumor xenograft model mice. A series of kinase assays showed that compound 17b inhibited various kinases including FAK, ACK1, FGFR, RSK1, IGF-1R, among others, thus demonstrating its potential for synergistic anti-tumor activity and development as a multi-targeted non-small cell lung cancer (NSCLC) therapy.