title: Sulphonamido-quinoxalines: search for anticancer agent.
abstract: A series of new sulphonamido-quinoxaline derivatives 3(a-p) have been prepared which are structurally similar to the High Throughput Screening (HTS) hit identified by Porter and collaborator. The newly synthesized compounds 3b, 3c, 3f, 3i, 3j, 3l, 3n and 3o were further evaluated in the National Cancer Institute for in vitro cytotoxicity assay among them compound 3l showed highest activity against Leukemia RPMI-8226 cell lines (GI50: 1.11 μM) as compared to other tested compounds. It is to be noted that compound 3l shows significant activity (GI50: 1.11 μM) compared to the High Throughput Screening (HTS) hit identified by Porter and collaborator (IC50 = 1.3 μM). Further docking study confirms the c-Met kinase inhibitory mechanism of the synthesized compounds.
authors.affiliation: Department of Pharmaceutical Chemistry, R.C. Patel College of Pharmacy, Shirpur, Dhule 425405, Maharashtra, India.
authors.forename: Rahul
authors.initials: R
authors.lastname: Ingle
authors.forename: Rajendra
authors.initials: R
authors.lastname: Marathe
authors.forename: Dipak
authors.initials: D
authors.lastname: Magar
authors.forename: Harun M
authors.initials: HM
authors.lastname: Patel
authors.forename: Sanjay J
authors.initials: SJ
authors.lastname: Surana
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D057166:High-Throughput Screening Assays; D006801:Humans; D015394:Molecular Structure; D011810:Quinoxalines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D011810:Quinoxalines; D013449:Sulfonamides
keywords: Anticancer; Docking; Lipinski's rule; Synthesis sulphonamido-quinoxaline