90919-75-8Relevant academic research and scientific papers
Novel non-ATP competitive small molecules targeting the CK2 α/β interface
Brear, Paul,North, Andrew,Iegre, Jessica,Hadje Georgiou, Kathy,Lubin, Alexandra,Carro, Laura,Green, William,Sore, Hannah F.,Hyv?nen, Marko,Spring, David R.
supporting information, p. 3016 - 3020 (2018/05/26)
Increased CK2 levels are prevalent in many cancers. Combined with the critical role CK2 plays in many cell-signaling pathways, this makes it a prime target for down regulation to fight tumour growth. Herein, we report a fragment-based approach to inhibiting the interaction between CK2α and CK2β at the α-β interface of the holoenzyme. A fragment, CAM187, with an IC50 of 44 μM and a molecular weight of only 257 gmol?1 has been identified as the most promising compound. Importantly, the lead fragment only bound at the interface and was not observed in the ATP binding site of the protein when co-crystallised with CK2α. The fragment-like molecules discovered in this study represent unique scaffolds to CK2 inhibition and leave room for further optimisation.
Synthesis and algicidal activity of new dichlorobenzylamine derivatives against harmful red tides
Choi, Dubok,Yu, Sunjong,Baek, Seung Ho,Kang, Yoon-Ho,Chang, Young-Cheol,Cho, Hoon
, p. 463 - 476 (2016/07/30)
In the present study, we synthesized 65 dichlorobenzylamine derivatives and investigated their algicidal activity against harmful red tides. The 3,4-dichlorobenzylamine derivatives showed relatively high activity against Cochlodinium polykrikoides, Heterosigma akashiwo, Chattonella marina, and Heterocapsa circularisquama, and the synthesized compounds 27, 28, 33, 34, 35, and 36 showed the highest algicidal activity after 24 h at 0.1 ~ 1.0 μM LC50 against the four harmful algae species. To verify the safety of the compounds, acute ecotoxicology tests using the water flea (Daphnia magna) and zebrafish (Danio rerio) were conducted, and the tests confirmed that compounds 33 and 34 were not harmful because the target organisms showed high survival rates at 15 μM. The results indicate that compounds 33 and 34 are suitable substances for use in controlling harmful algae species.
