Literature DB >> 17911019

Novel scaffold for cathepsin K inhibitors.

Naoki Teno1, Takahiro Miyake, Takeru Ehara, Osamu Irie, Junichi Sakaki, Osamu Ohmori, Hiroki Gunji, Naoko Matsuura, Keiichi Masuya, Yuko Hitomi, Kazuhiko Nonomura, Miyuki Horiuchi, Keigo Gohda, Atsuko Iwasaki, Ichiro Umemura, Sachiyo Tada, Motohiko Kometani, Genji Iwasaki, Sandra W Cowan-Jacob, Martin Missbach, René Lattmann, Claudia Betschart.   

Abstract

Pyrrolopyrimidine, a novel scaffold, allows to adjust interactions within the S3 subsite of cathepsin K. The core intermediate 10 facilitated the P3 optimization and identified highly potent and selective cathepsin K inhibitors 11-20.

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Year:  2007        PMID: 17911019     DOI: 10.1016/j.bmcl.2007.09.047

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


  6 in total

Review 1.  Nitrile-containing pharmaceuticals: efficacious roles of the nitrile pharmacophore.

Authors:  Fraser F Fleming; Lihua Yao; P C Ravikumar; Lee Funk; Brian C Shook
Journal:  J Med Chem       Date:  2010-08-30       Impact factor: 7.446

2.  Carbon-11 labeled cathepsin K inhibitors: syntheses and preliminary in vivo evaluation.

Authors:  Melissa E Rodnick; Xia Shao; Kenneth M Kozloff; Peter J H Scott; Michael R Kilbourn
Journal:  Nucl Med Biol       Date:  2014-02-18       Impact factor: 2.408

3.  Synthesis, characterization and molecular docking studies of thiouracil derivatives as potent thymidylate synthase inhibitors and potential anticancer agents.

Authors:  Abeer M El-Naggar; Mohsen M Abou-El-Regal; Souad A El-Metwally; Farag F Sherbiny; Ibrahim H Eissa
Journal:  Mol Divers       Date:  2017-08-16       Impact factor: 2.943

4.  Predicting the reactivity of nitrile-carrying compounds with cysteine: a combined computational and experimental study.

Authors:  Anna Berteotti; Federica Vacondio; Alessio Lodola; Michele Bassi; Claudia Silva; Marco Mor; Andrea Cavalli
Journal:  ACS Med Chem Lett       Date:  2014-02-24       Impact factor: 4.345

5.  Multicomponent mapping of boron chemotypes furnishes selective enzyme inhibitors.

Authors:  Joanne Tan; Armand B Cognetta Iii; Diego B Diaz; Kenneth M Lum; Shinya Adachi; Soumajit Kundu; Benjamin F Cravatt; Andrei K Yudin
Journal:  Nat Commun       Date:  2017-11-24       Impact factor: 14.919

Review 6.  Advances in the discovery of cathepsin K inhibitors on bone resorption.

Authors:  Jun Lu; Maolin Wang; Ziyue Wang; Zhongqi Fu; Aiping Lu; Ge Zhang
Journal:  J Enzyme Inhib Med Chem       Date:  2018-12       Impact factor: 5.051

  6 in total

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