39911-86-9Relevant academic research and scientific papers
Design, synthesis and pharmacophoric model building of new 3-alkoxymethyl/3-phenyl indole-2-carboxamides with potential antiproliferative activity
Abdelrahman, Mostafa H.,Aboraia, Ahmed S.,Youssif, Bahaa G. M.,Elsadek, Bakheet E. M.
, p. 64 - 82 (2017)
Novel 3-alkoxymethyl/3-phenyl indole-2-carboxamide derivatives were synthesized and evaluated for their anticancer activity. Most of the tested compounds showed moderate to excellent activity against the tested cell lines (MCF7 and HCT116). 3-Phenyl substitution on indole with p-piperidinyl phenethyl 24a and p-dimethylamino phenethyl 24c exhibited anticancer activity against MCF7 with IC50 of 0.13 and 0.14?μm, respectively. Further mechanistic study of the most active compounds through their action on cell cycle showed disturbance in cell cycle progression and cell cycle arrest. For future development of this series of compounds, pharmacophore study was conducted which indicated that the enhancement of the activity could be achieved through the addition of acceptor or donating groups to the already-present indole nucleus.
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.
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 (2007/10/03)
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
Potential antiinflammatory compounds. I. Antiinflammatory phenylpiperidine derivatives
Hicks,Smith,Williamson,Day
, p. 1460 - 1464 (2007/10/05)
The syntheses of a number of amines and their derivatives, based on the phenylpiperidine nucleus, are described. Their activities on the rat paw carrageenan test are also reported. Activities comparable to that of phenylbutazone were obtained for some of
