Literature DB >> 23036335

Homo- and heterodimeric Smac mimetics/IAP inhibitors as in vivo-active pro-apoptotic agents. Part I: Synthesis.

Leonardo Manzoni1, Laura Belvisi, Aldo Bianchi, Annalisa Conti, Carmelo Drago, Marilenia de Matteo, Luca Ferrante, Eloise Mastrangelo, Paola Perego, Donatella Potenza, Carlo Scolastico, Federica Servida, Gabriele Timpano, Francesca Vasile, Vincenzo Rizzo, Pierfausto Seneci.   

Abstract

Novel pro-apoptotic, homo- and heterodimeric Smac mimetics/IAPs inhibitors based on the N-AVPI-like 4-substituted 1-aza-2-oxobicyclo[5.3.0]decane scaffold were prepared from monomeric structures connected through a head-head (8), tail-tail (9) or head-tail (10) linker. The selection of appropriate decorating functions for the scaffolds, and of rigid and flexible linkers connecting them, is described. The synthesis, purification and analytical characterization of each prepared dimer 8-10 is thoroughly described.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 23036335     DOI: 10.1016/j.bmc.2012.09.020

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  7 in total

1.  Structural insight into inhibitor of apoptosis proteins recognition by a potent divalent smac-mimetic.

Authors:  Federica Cossu; Mario Milani; Patrice Vachette; Francesca Malvezzi; Serena Grassi; Daniele Lecis; Domenico Delia; Carmelo Drago; Pierfausto Seneci; Martino Bolognesi; Eloise Mastrangelo
Journal:  PLoS One       Date:  2012-11-15       Impact factor: 3.240

2.  Oncogenic KRAS sensitizes premalignant, but not malignant cells, to Noxa-dependent apoptosis through the activation of the MEK/ERK pathway.

Authors:  Annalisa Conti; Maria Teresa Majorini; Richard Elliott; Alan Ashworth; Christopher J Lord; Carlotta Cancelliere; Alberto Bardelli; Pierfausto Seneci; Henning Walczak; Domenico Delia; Daniele Lecis
Journal:  Oncotarget       Date:  2015-05-10

Review 3.  Inducing death in tumor cells: roles of the inhibitor of apoptosis proteins.

Authors:  Darren Finlay; Peter Teriete; Mitchell Vamos; Nicholas D P Cosford; Kristiina Vuori
Journal:  F1000Res       Date:  2017-04-27

4.  Selective Hydrogenation of Nitriles to Primary Amines Catalyzed by a Polysilane/SiO2-Supported Palladium Catalyst under Continuous-Flow Conditions.

Authors:  Yuki Saito; Haruro Ishitani; Masaharu Ueno; Shū Kobayashi
Journal:  ChemistryOpen       Date:  2017-01-23       Impact factor: 2.911

5.  Smac mimetics induce inflammation and necrotic tumour cell death by modulating macrophage activity.

Authors:  D Lecis; M De Cesare; P Perego; A Conti; E Corna; C Drago; P Seneci; H Walczak; M P Colombo; D Delia; S Sangaletti
Journal:  Cell Death Dis       Date:  2013-11-14       Impact factor: 8.469

6.  EGFR-targeted TRAIL and a Smac mimetic synergize to overcome apoptosis resistance in KRAS mutant colorectal cancer cells.

Authors:  Yvonne Möller; Martin Siegemund; Sven Beyes; Ricarda Herr; Daniele Lecis; Domenico Delia; Roland Kontermann; Tilman Brummer; Klaus Pfizenmaier; Monilola A Olayioye
Journal:  PLoS One       Date:  2014-09-08       Impact factor: 3.240

7.  Investigation of Hot Spot Region in XIAP Inhibitor Binding Site by Fragment Molecular Orbital Method.

Authors:  Hocheol Lim; Xuemei Jin; Jongwan Kim; Sungbo Hwang; Ki Beom Shin; Jiwon Choi; Ky-Youb Nam; Kyoung Tai No
Journal:  Comput Struct Biotechnol J       Date:  2019-08-21       Impact factor: 7.271

  7 in total

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