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Design, synthesis and pharmacophoric model building of new 3‐alkoxymethyl/3‐phenyl indole‐2‐carboxamides with potential antiproliferative activity
Author(s) -
Abdelrahman Mostafa H.,
Aboraia Ahmed S.,
Youssif Bahaa G. M.,
Elsadek Bakheet E. M.
Publication year - 2017
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12928
Subject(s) - indole test , pharmacophore , chemistry , carboxamide , stereochemistry , cell cycle checkpoint , cell cycle , cell , biochemistry
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 ( MCF 7 and HCT 116). 3‐Phenyl substitution on indole with p ‐piperidinyl phenethyl 24a and p ‐dimethylamino phenethyl 24c exhibited anticancer activity against MCF 7 with IC 50 of 0.13 and 0.14 μ m , 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.