Literature DB >> 21723120

Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors.

Marina Caldarelli1, Mauro Angiolini, Teresa Disingrini, Daniele Donati, Marco Guanci, Stefano Nuvoloni, Helena Posteri, Francesca Quartieri, Marco Silvagni, Riccardo Colombo.   

Abstract

The synthesis and SAR of a series of novel pyrazolo-quinazolines as potent and selective MPS1 inhibitors are reported. We describe the optimization of the initial hit, identified by screening the internal library collection, into an orally available, potent and selective MPS1 inhibitor.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID： 21723120     DOI： 10.1016/j.bmcl.2011.05.122

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


  10 in total

1.  Discovery of Pyrazolo[1,5-a]pyrimidine TTK Inhibitors: CFI-402257 is a Potent, Selective, Bioavailable Anticancer Agent.

Authors:  Yong Liu; Radoslaw Laufer; Narendra Kumar Patel; Grace Ng; Peter B Sampson; Sze-Wan Li; Yunhui Lang; Miklos Feher; Richard Brokx; Irina Beletskaya; Richard Hodgson; Olga Plotnikova; Donald E Awrey; Wei Qiu; Nickolay Y Chirgadze; Jacqueline M Mason; Xin Wei; Dan Chi-Chia Lin; Yi Che; Reza Kiarash; Graham C Fletcher; Tak W Mak; Mark R Bray; Henry W Pauls
Journal:  ACS Med Chem Lett       Date:  2016-05-06       Impact factor: 4.345

2.  Catalyst-free synthesis of quinazolin-4-ones from (hetero)aryl-guanidines: application to the synthesis of pyrazolo[4,3-f]quinazolin-9-ones, a new family of DYRK1A inhibitors.

Authors:  Julien Debray; Simon Bonte; Olivier Lozach; Laurent Meijer; Martine Demeunynck
Journal:  Mol Divers       Date:  2012-09-19       Impact factor: 2.943

3.  Diaminopyridine-based potent and selective mps1 kinase inhibitors binding to an unusual flipped-Peptide conformation.

Authors:  Ken-Ichi Kusakabe; Nobuyuki Ide; Yataro Daigo; Takeshi Itoh; Kenichi Higashino; Yousuke Okano; Genta Tadano; Yuki Tachibana; Yuji Sato; Makiko Inoue; Tooru Wada; Motofumi Iguchi; Takayuki Kanazawa; Yukichi Ishioka; Keiji Dohi; Sachie Tagashira; Yasuto Kido; Shingo Sakamoto; Kazuya Yasuo; Masahiro Maeda; Takahiko Yamamoto; Masayo Higaki; Takeshi Endoh; Kazuo Ueda; Takeshi Shiota; Hitoshi Murai; Yusuke Nakamura
Journal:  ACS Med Chem Lett       Date:  2012-06-06       Impact factor: 4.345

Review 4.  Applications of Palladium-Catalyzed C-N Cross-Coupling Reactions.

Authors:  Paula Ruiz-Castillo; Stephen L Buchwald
Journal:  Chem Rev       Date:  2016-09-30       Impact factor: 60.622

5.  Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1).

Authors:  Sébastien Naud; Isaac M Westwood; Amir Faisal; Peter Sheldrake; Vassilios Bavetsias; Butrus Atrash; Kwai-Ming J Cheung; Manjuan Liu; Angela Hayes; Jessica Schmitt; Amy Wood; Vanessa Choi; Kathy Boxall; Grace Mak; Mark Gurden; Melanie Valenti; Alexis de Haven Brandon; Alan Henley; Ross Baker; Craig McAndrew; Berry Matijssen; Rosemary Burke; Swen Hoelder; Suzanne A Eccles; Florence I Raynaud; Spiros Linardopoulos; Rob L M van Montfort; Julian Blagg
Journal:  J Med Chem       Date:  2013-12-02       Impact factor: 7.446

6.  Mps1 inhibitors synergise with low doses of taxanes in promoting tumour cell death by enhancement of errors in cell division.

Authors:  Ana Rita R Maia; Simon Linder; Ji-Ying Song; Chantal Vaarting; Ute Boon; Colin E J Pritchard; Arno Velds; Ivo J Huijbers; Olaf van Tellingen; Jos Jonkers; René H Medema
Journal:  Br J Cancer       Date:  2018-05-08       Impact factor: 7.640

7.  Scaffold-focused virtual screening: prospective application to the discovery of TTK inhibitors.

Authors:  Sarah R Langdon; Isaac M Westwood; Rob L M van Montfort; Nathan Brown; Julian Blagg
Journal:  J Chem Inf Model       Date:  2013-05-14       Impact factor: 4.956

8.  A meta analysis of pancreatic microarray datasets yields new targets as cancer genes and biomarkers.

Authors:  Nalin C W Goonesekere; Xiaosheng Wang; Lindsey Ludwig; Chittibabu Guda
Journal:  PLoS One       Date:  2014-04-16       Impact factor: 3.240

9.  CENPE, PRC1, TTK, and PLK4 May Play Crucial Roles in the Osteosarcoma Progression.

Authors:  Fei Wang; Qiheng Zhao; Wenping Liu; Daliang Kong
Journal:  Technol Cancer Res Treat       Date:  2020 Jan-Dec

10.  TTK inhibition increases cisplatin sensitivity in high-grade serous ovarian carcinoma through the mTOR/autophagy pathway.

Authors:  Gonghua Qi; Hanlin Ma; Yingwei Li; Jiali Peng; Jingying Chen; Beihua Kong
Journal:  Cell Death Dis       Date:  2021-12-07       Impact factor: 8.469
  10 in total

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