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Cytotoxicity and DNA binding property of triphenylethylene–coumarin hybrids with two amino side chains
- Source :
- Bioorganic & Medicinal Chemistry Letters. 24:900-904
- Publication Year :
- 2014
- Publisher :
- Elsevier BV, 2014.
-
Abstract
- Novel triphenylethylene–coumarin hybrids containing two amino side chains were designed and synthesized. Some of these 3,4-diphenyl coumarins, 7b – c (the double chains at 4-position on 3-,4-phenyl, respectively), and 13b – f (the double chains at 4-position on 3-phenyl and 7-position, respectively), showed a broad-spectrum and good anti-proliferative activity against five tumor cells and low cytotoxicity in osteoblast. UV–vis, fluorescence, and circular dichroism (CD) spectroscopies and thermal denaturation exhibited that compounds 7b (R = piperidinyl), 7e (R = NEt 2 ), and 7f (R = 4-methylpiperazinyl) had significant interactions with Ct-DNA by the intercalative mode of binding. Structure activity relationships (SARs) analysis suggested that the location of the two amino alkyl chains would play an important role both in the compounds against tumor cells proliferation and their interactions with DNA.
- Subjects :
- Circular dichroism
Cell Survival
Stereochemistry
Clinical Biochemistry
Pharmaceutical Science
Biochemistry
Structure-Activity Relationship
chemistry.chemical_compound
Coumarins
Cell Line, Tumor
Stilbenes
Drug Discovery
Side chain
Humans
Triphenylethylene
Amino Acids
Cytotoxicity
Molecular Biology
Alkyl
Cell Proliferation
chemistry.chemical_classification
Chemistry
Circular Dichroism
Organic Chemistry
DNA
Coumarin
Fluorescence
Drug Design
Molecular Medicine
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 24
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....abb66f351c89a5f9402d89d181ff7aef