Literature DB >> 12392735

Substituted benzocyloheptenes as potent and selective alpha(v) integrin antagonists.

Françoise Perron-Sierra1, Dominique Saint Dizier, Marc Bertrand, Annie Genton, Gordon C Tucker, Patrick Casara.   

Abstract

A novel series of potent and specific alpha(v) integrin antagonists has been obtained by aminoalkyl substitutions on benzocyloheptene acetic acids as a rigid GD bioisostere. The preferred compounds 1-2, 1-3 and 1-8, showed nano- to subnanomolar IC(50) values on alpha(v)beta(3) and alpha(v)beta(5) integrins, with favorable pharmacokinetics.

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Year:  2002        PMID： 12392735     DOI： 10.1016/s0960-894x(02)00696-0

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


  10 in total

1.  Nickel-Catalyzed [2+2+2] Cycloaddition of Diynes and Cyanamides.

Authors:  Ryan M Stolley; Michael T Maczka; Janis Louie
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2.  Reproducibility study of [(18)F]FPP(RGD)2 uptake in murine models of human tumor xenografts.

Authors:  Edwin Chang; Shuangdong Liu; Gayatri Gowrishankar; Shahriar Yaghoubi; James Patrick Wedgeworth; Frederick Chin; Dietmar Berndorff; Volker Gekeler; Sanjiv S Gambhir; Zhen Cheng
Journal:  Eur J Nucl Med Mol Imaging       Date:  2010-12-02       Impact factor: 9.236

3.  Inhibition of angiogenesis and tumor progression of MK-0429, an integrin αvβ3 antagonist, on oral squamous cell carcinoma.

Authors:  Takayuki Nakagawa; Kouji Ohta; Takako Naruse; Miyuki Sakuma; Syohei Fukada; Nao Yamakado; Misaki Akagi; Kazuki Sasaki; Chieko Niwata; Shigehiro Ono; Tomonao Aikawa
Journal:  J Cancer Res Clin Oncol       Date:  2022-06-17       Impact factor: 4.322

4.  Naturally occurring himachalenes to benzocycloheptene amino vinyl bromide derivatives: as antidepressant molecules.

Authors:  Abha Chaudhary; Pralay Das; Awanish Mishra; Pushpinder Kaur; Bikram Singh; Rajesh K Goel
Journal:  Mol Divers       Date:  2012-05-15       Impact factor: 2.943

5.  SAA1 polymorphisms are associated with variation in antiangiogenic and tumor-suppressive activities in nasopharyngeal carcinoma.

Authors:  H L Lung; O Y Man; M C Yeung; J M Y Ko; A K L Cheung; E W L Law; Z Yu; W H Shuen; E Tung; S H K Chan; D K Bangarusamy; Y Cheng; X Yang; R Kan; Y Phoon; K C Chan; D Chua; D L Kwong; A W M Lee; M F Ji; M L Lung
Journal:  Oncogene       Date:  2014-03-10       Impact factor: 9.867

6.  An inhibitor of a cell adhesion receptor stimulates cell migration.

Authors:  Shagufta H Shabbir; Jessica L Eisenberg; Milan Mrksich
Journal:  Angew Chem Int Ed Engl       Date:  2010-10-11       Impact factor: 15.336

Review 7.  One hundred years of benzotropone chemistry.

Authors:  Arif Dastan; Haydar Kilic; Nurullah Saracoglu
Journal:  Beilstein J Org Chem       Date:  2018-05-23       Impact factor: 2.883

8.  Stimulation of tumor growth and angiogenesis by low concentrations of RGD-mimetic integrin inhibitors.

Authors:  Andrew R Reynolds; Ian R Hart; Alan R Watson; Jonathan C Welti; Rita G Silva; Stephen D Robinson; Georges Da Violante; Morgane Gourlaouen; Mishal Salih; Matt C Jones; Dylan T Jones; Garry Saunders; Vassiliki Kostourou; Françoise Perron-Sierra; Jim C Norman; Gordon C Tucker; Kairbaan M Hodivala-Dilke
Journal:  Nat Med       Date:  2009-03-22       Impact factor: 53.440

9.  Alphav beta3 integrin limits the contribution of neuropilin-1 to vascular endothelial growth factor-induced angiogenesis.

Authors:  Stephen D Robinson; Louise E Reynolds; Vassiliki Kostourou; Andrew R Reynolds; Rita Graça da Silva; Bernardo Tavora; Marianne Baker; John F Marshall; Kairbaan M Hodivala-Dilke
Journal:  J Biol Chem       Date:  2009-10-16       Impact factor: 5.157

10.  Potential relevance of bell-shaped and u-shaped dose-responses for the therapeutic targeting of angiogenesis in cancer.

Authors:  Andrew R Reynolds
Journal:  Dose Response       Date:  2010-04-23       Impact factor: 2.658
  10 in total

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