Synthesis and evaluation of some new pyrazoline substituted benzenesulfonylureas as potential antiproliferative agents
| Autor: | Kalim Javed, Alhamzah Dh. Hameed, Mohammed Samim, Pooja Rathore, Rakesh Gupta, Shafiya Yaseen, Syed Ovais, Rafia Bashir, Raed Yaseen, Firasat Hussain |
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| Rok vydání: | 2013 |
| Předmět: |
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 |
| Zdroj: | Bioorganicmedicinal chemistry letters. 24(7) |
| ISSN: | 1464-3405 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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