Synthesis and evaluation of some new pyrazoline substituted benzenesulfonylureas as potential antiproliferative agents

• Published in: Bioorganic & medicinal chemistry letters Vol. 24; no. 7; pp. 1685 - 1691
• Main Authors: Rathore, Pooja, Yaseen, Shafiya, Ovais, Syed, Bashir, Rafia, Yaseen, Raed, Hameed, Alhamzah D., Samim, Mohammed, Gupta, Rakesh, Hussain, Firasat, Javed, Kalim
• Format: Journal Article
• Language: English
• Published: OXFORD Elsevier Ltd 01.04.2014; Elsevier
• Subjects: Anti-cancer; Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Antiproliferative activity; Benzenesulfonylureas; Cell Line, Tumor; Cell Proliferation - drug effects; Chemistry; Chemistry, Medicinal; Chemistry, Organic; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Humans; Life Sciences & Biomedicine; Molecular Structure; Pharmacology & Pharmacy; Physical Sciences; Pyrazoles - chemistry; Pyrazolines; Science & Technology; Structure-Activity Relationship; Sulfonamides; Sulfonylurea Compounds - chemical synthesis; Sulfonylurea Compounds - chemistry; Sulfonylurea Compounds - pharmacology; Benzenesulfonylureas; Anti-cancer; Antiproliferative activity; Sulfonamides; Pyrazolines; ANTICANCER AGENTS; DRUG DISCOVERY; BEARING BENZENE SULFONAMIDE; NATIONAL-CANCER-INSTITUTE; TUMORS; ANTITUMOR AGENTS; IN-VITRO; SCREEN; INHIBITORS; DERIVATIVES
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2014.02.059

Twenty six new pyrazoline substituted benzenesulfonylurea derivatives (2a–z) were synthesized and characterized. Out of these fourteen derivatives (2i, 2k–2p, 2r, 2s–2x) were evaluated for their antiproliferative activity towards 60 human cancer cell lines. 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 100μM). The compounds 2i, 2n, 2v and 2x showed effective growth inhibition (GI50 MID) values of 2.62, 3.93, 3.33, 3.74μM respectively beside cytostatic activity TGI (MG-MID) values of 8.42, 65.80, 24.00 and 36.06μM respectively. The compound 2i displayed remarkable antiproliferative activity in 8 different cell lines with GI50 less than 2μM. Compounds 2n, 2v and 2x also displayed good antiproliferative activity against 11, 18 and 14 different cell lines respectively with GI50 less than 3μM.