title: Design and synthesis of novel 1,2,3-triazole derivatives of coronopilin as anti-cancer compounds.
abstract: A series of 1,2,3-triazole coronopilin congeners have been designed and synthesized by employing click chemistry approach starting from parthenin and evaluated for their cytotoxicity against a panel of six human cancer cell lines (PC-3, THP-1, HCT-15, HeLa, A-549 and MCF-7). While many compounds exhibited significant anticancer activity, compound 3a, was found to be the most promising analogue in this series with IC50 values of 3.1 μM on PC-3 cell line. Flow-cytometric studies showed that 1,2,3-triazole derivative-3a induce dose dependent apoptosis in the sub G1 phase. This lead molecule-3a was further studied for NF-κB (p65) transcription factor inhibitory activity using Elisa and western blotting analysis which confirmed concentration dependent inhibitory activity against NF-κB, p65 with 80% inhibition in 24 h at 100 μM.
authors.affiliation: Medicinal Chemistry Division, CSIR - Indian Institute of Integrative Medicine, Jammu 180001, India.
authors.forename: Jabeena
authors.initials: J
authors.lastname: Khazir
authors.affiliation: Natural Products Chemistry Division, CSIR - Indian Institute of Chemical Technology, Hyderabad 500007, India.
authors.forename: Irfan
authors.initials: I
authors.lastname: Hyder
authors.affiliation: Natural Products Chemistry Division, CSIR - Indian Institute of Chemical Technology, Hyderabad 500007, India.
authors.forename: J Laxmi
authors.initials: JL
authors.lastname: Gayatri
authors.affiliation: Natural Products Chemistry Division, CSIR - Indian Institute of Chemical Technology, Hyderabad 500007, India.
authors.forename: Leela
authors.initials: L
authors.lastname: Prasad Yandrati
authors.affiliation: Natural Products Chemistry Division, CSIR - Indian Institute of Chemical Technology, Hyderabad 500007, India.
authors.forename: Naresh
authors.initials: N
authors.lastname: Nalla
authors.affiliation: Medicinal Chemistry Division, CSIR - Indian Institute of Integrative Medicine, Jammu 180001, India.
authors.forename: Gousia
authors.initials: G
authors.lastname: Chasoo
authors.affiliation: Medicinal Chemistry Division, CSIR - Indian Institute of Integrative Medicine, Jammu 180001, India.
authors.forename: Ajay
authors.initials: A
authors.lastname: Mahajan
authors.affiliation: Medicinal Chemistry Division, CSIR - Indian Institute of Integrative Medicine, Jammu 180001, India.
authors.forename: A K
authors.initials: AK
authors.lastname: Saxena
authors.affiliation: Department of Chemistry, Jamia Hamdard University, New Delhi 110062, India.
authors.forename: M S
authors.initials: MS
authors.lastname: Alam
authors.affiliation: Department of Chemistry, Jamia Hamdard University, New Delhi 110062, India.
authors.forename: G N
authors.initials: GN
authors.lastname: Qazi
authors.affiliation: Natural Products Chemistry Division, CSIR - Indian Institute of Chemical Technology, Hyderabad 500007, India. Electronic address: sampath@iict.res.in.
authors.forename: Halmuthur M
authors.initials: HM
authors.lastname: Sampath Kumar
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D052176:Azulenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells; D006801:Humans; D061986:MCF-7 Cells; D015394:Molecular Structure; D012717:Sesquiterpenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D052176:Azulenes; D012717:Sesquiterpenes; D014230:Triazoles; C584613:coronopilin
keywords: 1,2,3-Triazole; Coronopilin; NF-κB (p65) inhibitors; Parthenin; Sesquiterpenoid lactone