Kwiatkowski, Jacek’s team published research in Journal of Medicinal Chemistry in 2020-01-23 | 112253-70-0

Journal of Medicinal Chemistry published new progress about Antitumor agents. 112253-70-0 belongs to class amides-buliding-blocks, and the molecular formula is C7H7BrN2O, Name: 2-Amino-4-bromobenzamide.

Kwiatkowski, Jacek; Liu, Boping; Pang, Shermaine; Binte Ahmad, Nur Huda; Wang, Gang; Poulsen, Anders; Yang, Haiyan; Poh, Yong Rui; Tee, Doris Hui Ying; Ong, Esther; Retna, Priya; Dinie, Nurul; Kwek, Perlyn; Wee, John Liang Kuan; Manoharan, Vithya; Low, Choon Bing; Seah, Peck Gee; Pendharkar, Vishal; Sangthongpitag, Kanda; Joy, Joma; Baburajendran, Nithya; Jansson, Anna Elisabet; Nacro, Kassoum; Hill, Jeffrey; Keller, Thomas H.; Hung, Alvin W. published the artcile< Stepwise Evolution of Fragment Hits against MAPK Interacting Kinases 1 and 2>, Name: 2-Amino-4-bromobenzamide, the main research area is pyridine benzamide preparation mitogen protein kinase pharmacokinetic SAR docking.

Dysregulation of translation initiation factor 4E (eIF4E) activity occurs in various cancers. Mitogen-activated protein kinase (MAPK) interacting kinases 1 and 2 (MNK1 and MNK2) play a fundamental role in activation of eIF4E. Structure-activity relationship-driven expansion of a fragment hit led to discovery of dual MNK1 and MNK2 inhibitors based on a novel pyridine-benzamide scaffold. The compounds possess promising in vitro and in vivo pharmacokinetic profiles and show potent on target inhibition of eIF4E phosphorylation in cells.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 112253-70-0 belongs to class amides-buliding-blocks, and the molecular formula is C7H7BrN2O, Name: 2-Amino-4-bromobenzamide.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics