title: "Click" reaction mediated synthesis of costunolide and dehydrocostuslactone derivatives and evaluation of their cytotoxic activity.
abstract: As part of pharmacological-phytochemical integrated studies on medicinal plants from Indian flora, costunolide (1) and dehydrocostus lactone (2), were isolated as major phytochemicals from Saussurea lappa, a plant traditionally used in different Asian systems of medicine. A series of 1,4-disubstituted-1,2,3-triazoles conjugates were synthesized through diastereo selective Michael addition followed by regioselective Huisgen 1,3-dipolar cycloaddition reactions. All these triazolyl derivatives (5a-5j) & (7a-7j) were well characterized using modern spectroscopic techniques and evaluated for their anticancer activity against a panel of five human cancerous celllines. The results indicated that all the analogs displayed moderate cytotoxic activity.
authors.affiliation: a Division of Natural Products Chemistry , CSIR-Indian Institute of Chemical Technology , Hyderabad 500 607 , India.
authors.forename: Ch
authors.initials: Ch
authors.lastname: Pavan Kumar
authors.affiliation: a Division of Natural Products Chemistry , CSIR-Indian Institute of Chemical Technology , Hyderabad 500 607 , India.
authors.forename: A
authors.initials: A
authors.lastname: Devi
authors.affiliation: a Division of Natural Products Chemistry , CSIR-Indian Institute of Chemical Technology , Hyderabad 500 607 , India.
authors.forename: P
authors.initials: P
authors.lastname: Ashok Yadav
authors.affiliation: a Division of Natural Products Chemistry , CSIR-Indian Institute of Chemical Technology , Hyderabad 500 607 , India.
authors.forename: R
authors.initials: R
authors.lastname: Rao Vadaparthi
authors.affiliation: a Division of Natural Products Chemistry , CSIR-Indian Institute of Chemical Technology , Hyderabad 500 607 , India.
authors.forename: G
authors.initials: G
authors.lastname: Shankaraiah
authors.affiliation: b Centre for Chemical Biology , CSIR-Indian Institute of Chemical Technology , Hyderabad 500 607 , India.
authors.forename: P
authors.initials: P
authors.lastname: Sowjanya
authors.affiliation: b Centre for Chemical Biology , CSIR-Indian Institute of Chemical Technology , Hyderabad 500 607 , India.
authors.forename: Nishant
authors.initials: N
authors.lastname: Jain
authors.affiliation: a Division of Natural Products Chemistry , CSIR-Indian Institute of Chemical Technology , Hyderabad 500 607 , India.
authors.forename: K
authors.initials: K
authors.lastname: Suresh Babu
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007783:Lactones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D018517:Plant Roots / Q000737:chemistry; D010946:Plants, Medicinal / Q000737:chemistry; D030441:Saussurea / Q000737:chemistry*; D012717:Sesquiterpenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D007783:Lactones; D012717:Sesquiterpenes; C083030:dehydrocostus lactone; C002602:costunolide
keywords: Miachael addition; Saussurea lappa; costunolide; cytotoxic activity; dehydrococtuslactone