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Design, synthesis, and evaluation of novel heteroaromatic analogs of curcumin as anti-cancer agents
- Source :
- European Journal of Medicinal Chemistry. 75:123-131
- Publication Year :
- 2014
- Publisher :
- Elsevier BV, 2014.
-
Abstract
- To improve the potential of curcumin to treat advanced hormone-refractory prostate cancer, three series (A–C) of heteroaromatic analogs (thirty two compounds) with different monoketone linkers have been synthesized and evaluated for cytotoxicity against two human androgen-independent prostate cancer cell lines (PC-3 and DU-145). Among them, thirty analogs are more potent than curcumin against PC-3 cells, and twenty one analogs are more cytotoxic towards DU-145 cells relative to curcumin. The most potent compounds (44, 45, 51, and 52) also showed impressive cytotoxicity against three other metastatic cancer cell lines (MDA-MB-231, HeLa, and A549), with IC50 values ranging from 50 nM to 390 nM. All four most potent analogs exhibited no apparent cytotoxicity towards the MCF-10A normal mammary epithelial cells. Taken together, selective enhancement of cell death in prostate cancer cell lines and other aggressive cancer cell lines suggests that nitrogen-containing heteroaromatic rings are promising bioisosteres of the substituted phenyl ring in curcumin.
- Subjects :
- Male
Programmed cell death
Curcumin
Antineoplastic Agents
Pharmacology
Article
HeLa
chemistry.chemical_compound
Prostate cancer
Cell Line, Tumor
Neoplasms
Drug Discovery
medicine
Humans
Cytotoxic T cell
Cytotoxicity
Cell Death
biology
Organic Chemistry
Prostate
Prostatic Neoplasms
Cancer
General Medicine
biology.organism_classification
medicine.disease
chemistry
Cell culture
Drug Design
Drug Screening Assays, Antitumor
HeLa Cells
Subjects
Details
- ISSN :
- 02235234
- Volume :
- 75
- Database :
- OpenAIRE
- Journal :
- European Journal of Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....f8b27356e1d0279ea69d3a3f6dc2dd3f