Design, synthesis and pharmacophoric model building of new 3‐alkoxymethyl/3‐phenyl indole‐2‐carboxamides with potential antiproliferative activity

Abstract

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 IC 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 and Synthesis of (2-oxo-1,2-Dihydroquinolin-4-yl)-1,2,3-triazole Derivatives via Click Reaction: Potential Apoptotic Antiproliferative Agents

“…Following treatment with the most active compound, 8g, a cell cycle analysis was performed on the MCF-7 cancer cell line [33,34]. Figure 5 shows that the percentage of MCF-7 cell line cells in the G0/G1 phase was 53.61% in control and 36.25% after treatment with compound 8g, whereas the percentage of cells in the S phase was reduced with compound 8g (27.15%) compared to the control (42.01%).…”

Design and synthesis of new thiazolidinone/uracil derivatives as antiproliferative agents targeting EGFR and/or BRAFV600E

“…Using the MTT assay ( Abdelrahman et al, 2017 ; El-Sherief et al, 2018 ) and doxorubicin as the reference drug, 3a-f and 5a-l were tested for antiproliferative activity against four human cancer cell lines: Panc-1 (pancreas cancer cell line), MCF-7 (breast cancer cell line), HT-29 (colon cancer cell line), and A-549 (epithelial cancer cell line). The median inhibitory concentrations (IC 50 ) are shown in Table 4 .…”

Convenient synthesis, characterization and biological evaluation of novel 1-phenylcyclopropane carboxamide derivatives

“…Further, this cell viability was calculated for the inhibitory activity of compounds for these cells. Each dose was used to calculate the half-maximal inhibitory concentration (IC 50 ) by Graph Pad Prism software [ [25] , [26] , [25] ].…”