title: Novel Glycopyrrolidine Compounds Inhibit Human Cancer Cell Proliferation and Induce Apoptotic Mode of Cell Death.
abstract: Spirocyclic compounds, present in a number of bioactive natural alkaloids, are cyclic systems containing one carbon atom common to two rings. A highly regioselective glycopyrrolidine compound library was synthesized using 1,3-dipolar cycloaddition method, and its efficacy was tested on cell lines representing most commonly occurring cancers and the molecular mechanism of cell death deciphered. Results showed that among the 16 compounds screened, RPRR210 showed the most potent anticancer activity and induced cell cycle arrest, inhibited migration, caused cell death by inducing apoptosis through the intrinsic pathway, and were nontoxic to normal cells.
authors.affiliation: a Department of Human Genetics , Sri Ramachandra University , Porur , Chennai , India.
authors.forename: Hemadev
authors.initials: H
authors.lastname: Bhoopalan
authors.affiliation: b Department of Biotechnology , Indian Institute of Technology Madras (IITM) , Chennai , India.
authors.forename: Shilpa
authors.initials: S
authors.lastname: Tentu
authors.affiliation: c Department of Organic Chemistry , University of Madras , Guindy Campus , Chennai , India.
authors.forename: Prasana
authors.initials: P
authors.lastname: R
authors.affiliation: c Department of Organic Chemistry , University of Madras , Guindy Campus , Chennai , India.
authors.forename: Purushothaman
authors.initials: P
authors.lastname: S
authors.affiliation: a Department of Human Genetics , Sri Ramachandra University , Porur , Chennai , India.
authors.forename: Akkanapally
authors.initials: A
authors.lastname: Venu
authors.affiliation: c Department of Organic Chemistry , University of Madras , Guindy Campus , Chennai , India.
authors.forename: Ragavachary
authors.initials: R
authors.lastname: Raghunathan
authors.affiliation: d Indian Institute of Science Education & Research (IISER) , Tirupati , India.
authors.forename: Suresh Babu
authors.initials: SB
authors.lastname: Pakala
authors.affiliation: b Department of Biotechnology , Indian Institute of Technology Madras (IITM) , Chennai , India.
authors.forename: Suresh Kumar
authors.initials: SK
authors.lastname: Rayala
authors.affiliation: a Department of Human Genetics , Sri Ramachandra University , Porur , Chennai , India.
authors.forename: Ganesh
authors.initials: G
authors.lastname: Venkatraman
mesh_terms: D000072283:A549 Cells; D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D061986:MCF-7 Cells; D009369:Neoplasms / Q000188:drug therapy* / Q000473:pathology; D011759:Pyrrolidines / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D011759:Pyrrolidines
keywords: Glycopyrrolidines; anticancer activity; lung cancer; pancreatic cancer