title: Diminutive effect on T and B-cell proliferation of non-cytotoxic α-santonin derived 1,2,3-triazoles: a report.
abstract: α-Santonin derived new series of 1,2,3-triazoles synthesized through Azide-Alkyne Huisgen 1,3-dipolar cycloaddition reaction between substituted aryl azide and a propargylated α-desmotrosantonin were bio-evaluated for their diminutive effect on ConA induced T-cell and LPS induced B-cell proliferation. Interestingly, most of the synthesized compounds showed better immunosuppressant activity than α-santonin. Triazole derivatives 9, 10, 17, 18, 29, and 30 displayed significant diminutive effect on cell proliferation. Compounds 12 and 13 were found selective against ConA T-cell proliferation exhibiting >90% inhibition at 1 × 10(-6) M concentration. The present study resulted in identification of several triazole derivatives as effective immunosuppressive agents.
authors: Bioorganic Chemistry Division, CSIR-Indian Institute of Integrative Medicine, Canal Road, Jammu 180001, India.
authors: Praveen K
authors: PK
authors: Chinthakindi
authors: Payare L
authors: PL
authors: Sangwan
authors: Saleem
authors: S
authors: Farooq
authors: Rajeshwar R
authors: RR
authors: Aleti
authors: Anupurna
authors: A
authors: Kaul
authors: Ajit K
authors: AK
authors: Saxena
authors: Y L N
authors: YL
authors: Murthy
authors: Ram A
authors: RA
authors: Vishwakarma
authors: Surrinder
authors: S
authors: Koul
mesh_terms: D000818:Animals; D001402:B-Lymphocytes / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D003208:Concanavalin A / Q000494:pharmacology; D008070:Lipopolysaccharides / Q000494:pharmacology; D051379:Mice; D008807:Mice, Inbred BALB C; D015394:Molecular Structure; D012500:Santonin / Q000737:chemistry*; D013329:Structure-Activity Relationship; D013601:T-Lymphocytes / Q000187:drug effects; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D008070:Lipopolysaccharides; D014230:Triazoles; D003208:Concanavalin A; D012500:Santonin