title: Ligand-free Pd-catalyzed C-N cross-coupling/cyclization strategy: an unprecedented access to 1-thienyl pyrroloquinoxalines for the new approach towards apoptosis.
abstract: The link between PDE4 and apoptosis prompted us to design and synthesize for the first time a series of novel 1-thienyl pyrroloquinoxalines as potential PDE4 inhibitors/apoptotic agents. A ligand-free Pd-catalyzed C-N cross-coupling/cyclization strategy has been developed for the rapid and milder access to this class of compounds some of which showed interesting pharmacological properties when tested in vitro and in zebrafish embryos.
authors.affiliation: Department of Chemistry, Acharya Nagarjuna University, Nagarjuna Nagar, Guntur 522510, A.P., India.
authors.forename: Sunder Kumar
authors.initials: SK
authors.lastname: Kolli
authors.affiliation: Dr. Reddy's Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500046, India.
authors.forename: Ali
authors.initials: A
authors.lastname: Nakhi
authors.affiliation: Dr. Reddy's Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500046, India; Manipal College of Pharmaceutical Science, Manipal University, Manipal 576104, India.
authors.forename: Sivakumar
authors.initials: S
authors.lastname: Archana
authors.affiliation: Dr. Reddy's Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500046, India.
authors.forename: Maneesha
authors.initials: M
authors.lastname: Saridena
authors.affiliation: School of Pharmacy, University of Queensland, Brisbane QLD4072, Australia.
authors.forename: Girdhar Singh
authors.initials: GS
authors.lastname: Deora
authors.affiliation: Dr. Reddy's Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500046, India; Zephase Therapeutics (an incubated company at DRILS), University of Hyderabad Campus, Gachibowli, Hyderabad 500046, India.
authors.forename: Swapna
authors.initials: S
authors.lastname: Yellanki
authors.affiliation: Dr. Reddy's Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500046, India; Zephase Therapeutics (an incubated company at DRILS), University of Hyderabad Campus, Gachibowli, Hyderabad 500046, India.
authors.forename: Raghavender
authors.initials: R
authors.lastname: Medisetti
authors.affiliation: Dr. Reddy's Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500046, India; Zephase Therapeutics (an incubated company at DRILS), University of Hyderabad Campus, Gachibowli, Hyderabad 500046, India.
authors.forename: Pushkar
authors.initials: P
authors.lastname: Kulkarni
authors.affiliation: Department of Chemistry, Acharya Nagarjuna University, Nagarjuna Nagar, Guntur 522510, A.P., India.
authors.forename: R
authors.initials: R
authors.lastname: Ramesh Raju
authors.affiliation: Dr. Reddy's Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500046, India. Electronic address: manojitpal@rediffmail.com.
authors.forename: Manojit
authors.initials: M
authors.lastname: Pal
mesh_terms: D000818:Animals; D017209:Apoptosis / Q000187:drug effects*; D002384:Catalysis; D003500:Cyclization; D004305:Dose-Response Relationship, Drug; D015394:Molecular Structure; D010165:Palladium / Q000737:chemistry*; D058988:Phosphodiesterase 4 Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011758:Pyrroles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011810:Quinoxalines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015027:Zebrafish / Q000196:embryology
chemical_list: D058988:Phosphodiesterase 4 Inhibitors; D011758:Pyrroles; D011810:Quinoxalines; D013876:Thiophenes; D010165:Palladium
keywords: Apoptosis; PDE4; Palladium; Pyrroloquinoxaline; Zebrafish