title: Synthesis of new arylisoxazole-oxindole conjugates as potent antiproliferative agents.
abstract: A new series of arylisoxazole-oxindole derivatives (6a-r) were synthesized and evaluated for their antiproliferative activity against human cancer cell lines including non-small cell lung (A549), cervical (HeLa), breast (MCF-7), and prostate (DU-145) cancer cell lines. The synthesized compounds (6a-r) demonstrated excellent to moderate cytotoxicity with IC50values ranging from 0.82 to 3.69 μm. Some new compounds (6m-r) exhibited profound cytotoxicity better or similar to positive control. More particularly, the compound 6q possesses donating substituent like methoxy group presented at 5-position on D ring exhibited remarkable antiproliferative activity against A-549 (lung cancer) with an IC50value 0.82 μm. Further studies to determine the mechanistic aspects of these conjugates are under progress.
authors.affiliation: Department of Pharmaceutical Engineering, School of Chemistry, Chemical Engineering and Life Science, Wuhan University of Technology, Wuhan, China.
authors.forename: Gajjela Bharath
authors.initials: GB
authors.lastname: Kumar
authors.affiliation: Department of Pharmaceutical Engineering, School of Chemistry, Chemical Engineering and Life Science, Wuhan University of Technology, Wuhan, China.
authors.forename: Syed Nasir Abbas
authors.initials: SN
authors.lastname: Bukhari
authors.affiliation: Department of Pharmaceutical Engineering, School of Chemistry, Chemical Engineering and Life Science, Wuhan University of Technology, Wuhan, China.
authors.forename: Hua-Li
authors.initials: HL
authors.lastname: Qin
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007211:Indoles / Q000737:chemistry* / Q000494:pharmacology; D010080:Oxazoles / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D007211:Indoles; D010080:Oxazoles
keywords: antiproliferative activity; arylisoxazole-oxindole; cancer; drug discovery; nocodazole