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- W2741866564 abstract "Substituted 2-amino-7-((6-(4-(2-hydroxyethyl) piperazin-1-yl)-2-methylpyrimidin-4-yl)oxy)-4-phenyl-4H-chromene-3-carbonitriles and 2-amino-7-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)oxy)-4-phenyl-1,4-dihydroquinoline-3-carbonitriles were synthesized via an efficient multi-component one pot synthesis under mild conditions. These compounds 1–20 were evaluated against human breast cancer cell lines (MCF-7) and human embryonic kidney cells (HEK293) for cytotoxic activities. Among them, compounds 6, 7, 15, 17 and 19 showed better anti-proliferative activities as (IC50 value 48 ± 1.70, 65 ± 1.13, 92 ± 1.18, 30 ± 1.17 and 16 ± 1.10 µM) than curcumin drug (48 ± 1.11 µM). Molecular docking was also performed with active compounds 6, 7 and 15 against Bcl-2 protein which gave good binding affinity (ΔG = −9.08, −8.29 and −7.70 kcal/mol) respectively. Furthermore, the structure-activity relationship (SAR) analysis revealed that the chromene and quinoline moieties, when attached with pyrimide and piperazine moieties, enhanced anti-proliferative activities." @default.
- W2741866564 created "2017-08-08" @default.
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- W2741866564 date "2017-09-01" @default.
- W2741866564 modified "2023-10-10" @default.
- W2741866564 title "Synthesis, estrogen receptor binding affinity and molecular docking of pyrimidine-piperazine-chromene and -quinoline conjugates" @default.
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- W2741866564 doi "https://doi.org/10.1016/j.bmcl.2017.07.077" @default.
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