65389-81-3Relevant academic research and scientific papers
Design and synthesis of novel pyrrolo[2,3-b]pyridine derivatives targeting V600EBRAF
Abdel-Maksoud, Mohammed S.,Ali, Eslam M. H.,Ammar, Usama M.,Mersal, Karim I.,Oh, Chang-Hyun,Yoo, Kyung Ho
, (2020/04/28)
Several pyrrolo[2,3-b]pyridine-based B-RAF inhibitors are well known and some of them are currently FDA approved as anticancer agents. Based on the structure of these FDA approved V600EB-RAF inhibitors, two series of pyrrolo[2,3-b]pyridine scaffold were designed and synthesized in attempt to develop new potent V600EB-RAF inhibitors. The 38 synthesized compounds were biologically evaluated for their V600EB-RAF inhibitory effect at single dose (10 μM). Compounds with high percent inhibition were tested to determine their IC50 over V600EB-RAF. Compounds 34e and 35 showed the highest inhibitory effect with IC50 values of 0.085 μM and 0.080 μM, respectively. Headed for excessive biological evaluation, the synthesized derivatives were tested over sixty diverse human cancer cell lines. Only compound 35 emerged as a potent cytotoxic agent against different panel of human cancer cell lines.
Preparation method and applications of aromatic heterocyclic compound adopted as selective JAK3 and/or JAK1 kinase inhibitor
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Paragraph 0149-0152; 0453-0456, (2016/10/08)
The present invention relates to an aromatic heterocyclic compound, a preparation method and applications thereof, wherein the structure of the compound is represented by a general formula (I), each group is defined in the specification, and the compound
Highly diastereo- and enantioselective direct Barbas-List aldol reactions promoted by novel benzamidoethyl and benzamidopropyl prolinamides in water
Pedrosa, Rafael,Andres, Jose M.,Manzano, Ruben,Roman, David,Tellez, Silvia
supporting information; experimental part, p. 935 - 940 (2011/03/22)
Four novel benzamido-functionalized prolinamides have been prepared and tested as organocatalysts for enantioselective aldol reaction of aldehydes and cyclic ketones in water. In particular, prolinamide derived from achiral ethylene diamine was the best c
