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Synthesis and evaluation of some new pyrazoline substituted benzenesulfonylureas as potential antiproliferative agents
- Source :
- Bioorganicmedicinal chemistry letters. 24(7)
- Publication Year :
- 2013
-
Abstract
- Twenty six new pyrazoline substituted benzenesulfonylureas (2a–z) were synthesized and tested for in vitro anticancer activity. Fourteen derivatives (2i, 2k–2p, 2r, 2s–2x) were screened for their antiproliferative activity towards 60 human cancer cell lines by the National Cancer Institute (USA). Among them four compounds (2i, 2n, 2v and 2x) exhibited significant growth inhibition and further screened at 10-fold dilutions of five different concentrations (0.01, 0.1, 1, 10 and 100 μM). The compounds 2i, 2n, 2v and 2x showed effective growth inhibition (GI50 MID) values of 2.62, 3.93, 3.33, 3.74 μM respectively beside cytostatic activity TGI (MG-MID) values of 8.42, 65.80, 24.00 and 36.06 μM respectively. The compound 2i displayed remarkable antiproliferative activity in 8 different cell lines with GI50 less than 2 μM. Compounds 2n, 2v and 2x also displayed good antiproliferative activity against 11, 18 and 14 different cell lines respectively with GI50 less than 3 μM.
- Subjects :
- Stereochemistry
Clinical Biochemistry
Pharmaceutical Science
Pyrazoline
Antineoplastic Agents
Biochemistry
chemistry.chemical_compound
Structure-Activity Relationship
Cell Line, Tumor
Drug Discovery
medicine
Humans
Molecular Biology
Cell Proliferation
Dose-Response Relationship, Drug
Molecular Structure
Organic Chemistry
Cancer
medicine.disease
In vitro
Sulfonylurea Compounds
chemistry
Cell culture
Antiproliferative Agents
Molecular Medicine
Pyrazoles
Growth inhibition
Drug Screening Assays, Antitumor
Human cancer
Subjects
Details
- ISSN :
- 14643405
- Volume :
- 24
- Issue :
- 7
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....9e003baa8363b2da656650af550d00fb