175696-75-0Relevant academic research and scientific papers
The antiinfluenza activity of pyrrolo[2,3-d]pyrimidines
Sznaidman, Marcos L.,Meade, Eric A.,Beauchamp, Lilia M.,Russell, Stuart,Tisdale, Margaret
, p. 565 - 568 (1996)
From a group of pyrrolo[2,3-d]pyrimidine compounds that have been screened against influenza virus, one derivative, 4-(3-piperidinyl benzylamino)-2-methyl-7H-pyrrolo[2,3-d]pyrimidine (9), has shown promising activity against both the A and B strains. The
Design, synthesis, and biological evaluation of novel EGFR inhibitors containing 5-chloro-3-hydroxymethyl-indole-2-carboxamide scaffold with apoptotic antiproliferative activity
Mohamed, Fatma A.M.,Gomaa, Hesham A.M.,Hendawy,Ali, Asmaa T.,Farghaly, Hatem S.,Gouda, Ahmed M.,Abdelazeem, Ahmed H.,Abdelrahman, Mostafa H.,Trembleau, Laurent,Youssif, Bahaa G.M.
supporting information, (2021/05/26)
New EGFR inhibitor series of fifteen 5-chloro-3-hydroxymethyl-indole-2-carboxamide derivatives has been designed, synthesized, and tested for antiproliferative activity against a panel of cancer cell lines. The results showed that p-substituted phenethyl derivatives 10, 11, 13, 15 and 17–19 showed superior antiproliferative activity compared to their m-substituted counterparts 12, 14, 16 and 20. Compounds 15, 16, 19 and 20 displayed promising EGFR inhibitory activity as well as an increase in caspase 3 levels. Compounds 15 and 19 increased caspase-8 and 9 levels, as well as inducing Bax and decreasing Bcl-2 protein levels. Compound 19 demonstrated cell cycle arrest at pre-G1 and G2/M phases. The results of the docking study into the active site of EGFR revealed strong fitting of the new compounds with higher binding affinities compared to erlotinib.
