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Design and synthesis of dithiocarbamate linked β-carboline derivatives: DNA topoisomerase II inhibition with DNA binding and apoptosis inducing ability
- Source :
- Bioorganic & Medicinal Chemistry. 23:5511-5526
- Publication Year :
- 2015
- Publisher :
- Elsevier BV, 2015.
-
Abstract
- A series of new β-carboline-dithiocarbamate derivatives bearing phenyl, dithiocarbamate and H/methyl substitutions at position-1, 3 and 9, respectively, were designed and synthesized. These derivatives 8a-l and 13a-l and their starting precursors (7 a-d and 12 a-d) have been evaluated for their in vitro cytotoxic activity on selected human cancer cell lines. Among the derivatives tested, 7 c, 12 c, 8 a, 8 d, 8 i, 8 j, 8 k, 8l and 13 d-l exhibited considerable cytotoxicity against most of the tested cancer cell lines (IC50
- Subjects :
- Stereochemistry
Clinical Biochemistry
Pharmaceutical Science
Antineoplastic Agents
Apoptosis
Biochemistry
Structure-Activity Relationship
chemistry.chemical_compound
Drug Discovery
medicine
Humans
Topoisomerase II Inhibitors
Structure–activity relationship
Dithiocarbamate
Cytotoxicity
Molecular Biology
chemistry.chemical_classification
Molecular Structure
Organic Chemistry
DNA
In vitro
chemistry
Mechanism of action
Molecular Medicine
Topoisomerase-II Inhibitor
medicine.symptom
Carbolines
Subjects
Details
- ISSN :
- 09680896
- Volume :
- 23
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....664114db678d19bacd2fdd0f0e5662f2
- Full Text :
- https://doi.org/10.1016/j.bmc.2015.07.037