Synthesis, in-vitro screening, and docking analysis of novel pyrrolidine and piperidine-substituted ethoxy chalcone as anticancer agents

A series of novel-substituted chalcone analogs were synthesized and evaluated for antiproliferative activity against estrogen receptor-positive MCF-7 breast cancer cell lines. Among the synthesized derivatives 4a , 5a , 5b , 5c , 5e , 5′a , and 5′d show good antiproliferative activity as compared to...

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Published inMedicinal chemistry research Vol. 24; no. 5; pp. 1842 - 1856
Main Authors Mokale, Santosh N., Dube, Pritam N., Bhavale, Swati A., Sayed, Ibrahim, Begum, Afreen, Nevase, Manjusha C., Shelke, Vishakha R., Mujaheed, Abdul
Format Journal Article
LanguageEnglish
Published New York Springer US 01.05.2015
Subjects
Biochemistry
Biomedical and Life Sciences
Biomedicine
Cell Biology
Original Research
Pharmacology/Toxicology
Breast cancer
ADME
Chalcone
Molecular docking
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Summary:A series of novel-substituted chalcone analogs were synthesized and evaluated for antiproliferative activity against estrogen receptor-positive MCF-7 breast cancer cell lines. Among the synthesized derivatives 4a , 5a , 5b , 5c , 5e , 5′a , and 5′d show good antiproliferative activity as compared to standard tamoxifen. The study highlighted the advantage of introducing the amine side chain pharmacophore in substituted chalcone enhances the anticancer potential. The study also suggests that these analogs can serve as better therapeutic agents against breast cancer and can provide starting point for building more potent analogs in future. The binding mechanism and ADME properties of target compounds were analysed using Schrödinger software.
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-014-1266-8