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Structure-based Drug Design and Synthesis of PARP Inhibitors - Softcover

 
9786200437785: Structure-based Drug Design and Synthesis of PARP Inhibitors

Synopsis

Poly(ADP-ribose)polymerase (PARP) is a chromatin bound nuclear enzyme which gets activated by DNA breaks, uses NAD as substrate and catalyses the poly-ADP ribosylation of a variety of proteins. The enzyme PARP is considered as a suitable target for anti-cancer activity as it is involved in a variety of physiological functions like cellular proliferation, differentiation, apoptosis and DNA replication. Based on the literature, pharmacophoric templates and bio-isosteric replacement approach, quinazolinone and phthalazinone derivatives were selected to design molecules to calculate binding affinity and visualize binding conformations and interactions at the active pocket of target PARP-1 protein. For preliminary evaluation, in silico potential compounds were selected to synthesize, purified by column chromatography, characterized by HNMR and Mass Spectral studies and carried out for in vitro cytotoxicity. Molecular docking and preliminary experimental data helped to investigate Structure Activity Relationship for design of safe and potential PARP-1 inhibitors for cancer therapy.

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  • PublisherLAP Lambert Academic Publishing
  • Publication date2019
  • ISBN 10 6200437785
  • ISBN 13 9786200437785
  • BindingPaperback
  • LanguageEnglish
  • Number of pages108

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Manikanta Murahari
Published by LAP Lambert Academic Publishing, 2019
ISBN 10: 6200437785 ISBN 13: 9786200437785
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Taschenbuch. Condition: Neu. This item is printed on demand - it takes 3-4 days longer - Neuware -Poly(ADP-ribose)polymerase (PARP) is a chromatin bound nuclear enzyme which gets activated by DNA breaks, uses NAD as substrate and catalyses the poly-ADP ribosylation of a variety of proteins. The enzyme PARP is considered as a suitable target for anti-cancer activity as it is involved in a variety of physiological functions like cellular proliferation, differentiation, apoptosis and DNA replication. Based on the literature, pharmacophoric templates and bio-isosteric replacement approach, quinazolinone and phthalazinone derivatives were selected to design molecules to calculate binding affinity and visualize binding conformations and interactions at the active pocket of target PARP-1 protein. For preliminary evaluation, in silico potential compounds were selected to synthesize, purified by column chromatography, characterized by HNMR and Mass Spectral studies and carried out for in vitro cytotoxicity. Molecular docking and preliminary experimental data helped to investigate Structure Activity Relationship for design of safe and potential PARP-1 inhibitors for cancer therapy. 108 pp. Englisch. Seller Inventory # 9786200437785

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Manikanta Murahari
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Taschenbuch. Condition: Neu. nach der Bestellung gedruckt Neuware - Printed after ordering - Poly(ADP-ribose)polymerase (PARP) is a chromatin bound nuclear enzyme which gets activated by DNA breaks, uses NAD as substrate and catalyses the poly-ADP ribosylation of a variety of proteins. The enzyme PARP is considered as a suitable target for anti-cancer activity as it is involved in a variety of physiological functions like cellular proliferation, differentiation, apoptosis and DNA replication. Based on the literature, pharmacophoric templates and bio-isosteric replacement approach, quinazolinone and phthalazinone derivatives were selected to design molecules to calculate binding affinity and visualize binding conformations and interactions at the active pocket of target PARP-1 protein. For preliminary evaluation, in silico potential compounds were selected to synthesize, purified by column chromatography, characterized by HNMR and Mass Spectral studies and carried out for in vitro cytotoxicity. Molecular docking and preliminary experimental data helped to investigate Structure Activity Relationship for design of safe and potential PARP-1 inhibitors for cancer therapy. Seller Inventory # 9786200437785

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Condition: New. Dieser Artikel ist ein Print on Demand Artikel und wird nach Ihrer Bestellung fuer Sie gedruckt. Autor/Autorin: Murahari ManikantaDr. Manikanta Murahari is an academic researcher presently working as Assistant Professor at Department of Pharmaceutical Chemistry, Faculty of Pharmacy, M.S. Ramaiah University of Applied Sciences, Bangalore. He wo. Seller Inventory # 335816147

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Taschenbuch. Condition: Neu. Neuware -Poly(ADP-ribose)polymerase (PARP) is a chromatin bound nuclear enzyme which gets activated by DNA breaks, uses NAD as substrate and catalyses the poly-ADP ribosylation of a variety of proteins. The enzyme PARP is considered as a suitable target for anti-cancer activity as it is involved in a variety of physiological functions like cellular proliferation, differentiation, apoptosis and DNA replication. Based on the literature, pharmacophoric templates and bio-isosteric replacement approach, quinazolinone and phthalazinone derivatives were selected to design molecules to calculate binding affinity and visualize binding conformations and interactions at the active pocket of target PARP-1 protein. For preliminary evaluation, in silico potential compounds were selected to synthesize, purified by column chromatography, characterized by HNMR and Mass Spectral studies and carried out for in vitro cytotoxicity. Molecular docking and preliminary experimental data helped to investigate Structure Activity Relationship for design of safe and potential PARP-1 inhibitors for cancer therapy.Books on Demand GmbH, Überseering 33, 22297 Hamburg 108 pp. Englisch. Seller Inventory # 9786200437785

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