Literature DB >> 15603957

A novel series of potent gamma-secretase inhibitors based on a benzobicyclo[4.2.1]nonane core.

Stephen J Lewis1, Adrian L Smith, Joseph G Neduvelil, Graeme I Stevenson, Matthew J Lindon, A Brian Jones, Mark S Shearman, Dirk Beher, Earl Clarke, Jonathan D Best, James E Peachey, Timothy Harrison, J Luis Castro.   

Abstract

A new series of gamma-secretase inhibitors was developed from an in-house screening hit based on a benzobicyclo[4.2.1]nonane core. Lead optimisation studies led to the development of a series of potent inhibitors and in vivo efficacy was demonstrated.

Entities:  

Mesh:

Substances:

Year:  2005        PMID: 15603957     DOI: 10.1016/j.bmcl.2004.10.062

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  11 in total

1.  Notch signaling is not essential in sonic hedgehog-activated medulloblastoma.

Authors:  B A Hatton; E H Villavicencio; J Pritchard; M LeBlanc; S Hansen; M Ulrich; S Ditzler; B Pullar; M R Stroud; J M Olson
Journal:  Oncogene       Date:  2010-05-03       Impact factor: 9.867

2.  In vivo manifestation of Notch related phenotypes in zebrafish treated with Alzheimer's amyloid reducing gamma-secretase inhibitors.

Authors:  Ting Yang; Dilyara Arslanova; Xiaoyin Xu; Yue-Ming Li; Weiming Xia
Journal:  J Neurochem       Date:  2010-03-12       Impact factor: 5.372

3.  Rationalizing lead optimization by consensus 2D- CoMFA CoMSIA GRIND (3D) QSAR guided fragment hopping in search of γ-secretase inhibitors.

Authors:  Prabu Manoharan; Nanda Ghoshal
Journal:  Mol Divers       Date:  2012-08-14       Impact factor: 2.943

4.  Arc/Arg3.1 regulates an endosomal pathway essential for activity-dependent β-amyloid generation.

Authors:  Jing Wu; Ronald S Petralia; Hideaki Kurushima; Hiral Patel; Mi-young Jung; Lenora Volk; Shoaib Chowdhury; Jason D Shepherd; Marlin Dehoff; Yueming Li; Dietmar Kuhl; Richard L Huganir; Donald L Price; Robert Scannevin; Juan C Troncoso; Philip C Wong; Paul F Worley
Journal:  Cell       Date:  2011-10-28       Impact factor: 41.582

Review 5.  Notch inhibition as a promising new approach to cancer therapy.

Authors:  Benjamin Purow
Journal:  Adv Exp Med Biol       Date:  2012       Impact factor: 2.622

6.  gamma-Secretase inhibitors abrogate oxaliplatin-induced activation of the Notch-1 signaling pathway in colon cancer cells resulting in enhanced chemosensitivity.

Authors:  Raymond D Meng; Christopher C Shelton; Yue-Ming Li; Li-Xuan Qin; Daniel Notterman; Philip B Paty; Gary K Schwartz
Journal:  Cancer Res       Date:  2009-01-15       Impact factor: 12.701

7.  NOTCH pathway blockade depletes CD133-positive glioblastoma cells and inhibits growth of tumor neurospheres and xenografts.

Authors:  Xing Fan; Leila Khaki; Thant S Zhu; Mary E Soules; Caroline E Talsma; Naheed Gul; Cheryl Koh; Jiangyang Zhang; Yue-Ming Li; Jarek Maciaczyk; Guido Nikkhah; Francesco Dimeco; Sara Piccirillo; Angelo L Vescovi; Charles G Eberhart
Journal:  Stem Cells       Date:  2010-01       Impact factor: 6.277

8.  Ligand-dependent Notch signaling is involved in tumor initiation and tumor maintenance in pancreatic cancer.

Authors:  Michael E Mullendore; Jan-Bart Koorstra; Yue-Ming Li; G Johan Offerhaus; Xing Fan; Clark M Henderson; William Matsui; Charles G Eberhart; Anirban Maitra; Georg Feldmann
Journal:  Clin Cancer Res       Date:  2009-03-03       Impact factor: 12.531

Review 9.  Notch inhibitors as a new tool in the war on cancer: a pathway to watch.

Authors:  Benjamin Purow
Journal:  Curr Pharm Biotechnol       Date:  2009-02       Impact factor: 2.837

10.  Investigation on the Anticancer Activity of Symmetric and Unsymmetric Cyclic Sulfamides.

Authors:  Jaden Jungho Jun; Divya Duscharla; Ramesh Ummanni; Paul R Hanson; Sanjay V Malhotra
Journal:  ACS Med Chem Lett       Date:  2021-01-15       Impact factor: 4.345

View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.