title: Synthesis and anticancer activity of heteroaromatic linked 4β-amido podophyllotoxins as apoptotic inducing agents.
abstract: A series of different heteroaromatic linked 4β-amidopodophyllotoxin conjugates (16a-i, 17a-i and 18a-d) were synthesized and evaluated for anticancer activity against five human cancer cell lines. Among the series, one of the compound 17g showed significant antiproliferative activity in A549 (lung cancer) cell line. Flow cytometric analysis showed that 17g arrested the cell cycle in the G2/M phase leading to caspase-3 dependent apoptotic cell death. Further, Hoechst 33258 staining and DNA fragmentation assay also suggests that 17g induces cell death by apoptosis.
authors.affiliation: Division of Organic Chemistry, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, India. ahmedkamal@iict.res.in
authors.forename: Ahmed
authors.initials: A
authors.lastname: Kamal
authors.forename: Jaki R
authors.initials: JR
authors.lastname: Tamboli
authors.forename: M V P S
authors.initials: MV
authors.lastname: Vishnuvardhan
authors.forename: S F
authors.initials: SF
authors.lastname: Adil
authors.forename: V Lakshma
authors.initials: VL
authors.lastname: Nayak
authors.forename: S
authors.initials: S
authors.lastname: Ramakrishna
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity*; D017209:Apoptosis / Q000187:drug effects*; D053148:Caspase 3 / Q000378:metabolism; D045744:Cell Line, Tumor; D004247:DNA / Q000378:metabolism; D053938:DNA Fragmentation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D059565:G2 Phase Cell Cycle Checkpoints / Q000187:drug effects; D019073:HT29 Cells; D006367:HeLa Cells; D006571:Heterocyclic Compounds / Q000737:chemistry*; D006801:Humans; D059566:M Phase Cell Cycle Checkpoints / Q000187:drug effects; D051379:Mice; D011034:Podophyllotoxin / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity
chemical_list: D000970:Antineoplastic Agents; D006571:Heterocyclic Compounds; D004247:DNA; D053148:Caspase 3; D011034:Podophyllotoxin