Literature DB >> 16099651

Synthesis of some pyrazole derivatives and preliminary investigation of their affinity binding to P-glycoprotein.

Fedele Manna1, Franco Chimenti, Rossella Fioravanti, Adriana Bolasco, Daniela Secci, Paola Chimenti, Cristiano Ferlini, Giovanni Scambia.   

Abstract

A series of substituted pyrazolines were synthesized and evaluated for their anticancer activity and for their ability to inhibit P-glycoprotein-mediated multidrug resistance by direct binding to a purified protein domain containing an ATP-binding site and a modulator interacting region. Compounds 2a and e have been found to bind to P-glycoprotein with greater affinity.

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Year:  2005        PMID: 16099651     DOI: 10.1016/j.bmcl.2005.05.067

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


  16 in total

1.  Solution-phase parallel synthesis of a library of delta(2)-pyrazolines.

Authors:  Shankar Manyem; Mukund P Sibi; Gerald H Lushington; Benjamin Neuenswander; Frank Schoenen; Jeffrey Aubé
Journal:  J Comb Chem       Date:  2007 Jan-Feb

2.  Synthesis of 5-aryl-1,3-dimethyl-6-(alkyl- or aryl-amino) furo [2,3-d]pyrimidine derivatives by reaction between isocyanides and pyridinecarbaldehydes in the presence of 1,3-dimethylbarbituric acid.

Authors:  Malek Taher Maghsoodlou; Ghasem Marandi; Nourallah Hazeri; Sayyed Mostafa Habibi-Khorassani; Ali Akbar Mirzaei
Journal:  Mol Divers       Date:  2010-07-11       Impact factor: 2.943

3.  Prodrugs of a CXC Chemokine-12 (CXCL12) Neutraligand Prevent Inflammatory Reactions in an Asthma Model in Vivo.

Authors:  Vincent Gasparik; François Daubeuf; Muriel Hachet-Haas; François Rohmer; Patrick Gizzi; Jacques Haiech; Jean-Luc Galzi; Marcel Hibert; Dominique Bonnet; Nelly Frossard
Journal:  ACS Med Chem Lett       Date:  2011-12-09       Impact factor: 4.345

4.  1-[3,5-Bis(4-fluoro-phen-yl)-4,5-dihydro-1H-pyrazol-1-yl]ethanone.

Authors:  Hoong-Kun Fun; Madhukar Hemamalini; S Samshuddin; B Narayana; H S Yathirajan
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-02-10

5.  Reactivity of 4-tert-butyldimethylsiloxy-1,2,3,6-tetrahydropyridines with hydrazines.

Authors:  Javier Figueroa; Esther Caballero; Pilar Puebla; Fernando Tomé; Manuel Medarde
Journal:  Molecules       Date:  2006-11-30       Impact factor: 4.411

6.  3,5-Bis(4-meth-oxy-phen-yl)-1-phenyl-4,5-dihydro-1H-pyrazole.

Authors:  Zeliha Baktır; Mehmet Akkurt; S Samshuddin; B Narayana; H S Yathirajan
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-01-12

7.  Synthesis and Activity Evaluation of 2-(1-naphtho[2,1-b]furan-2-yl-carbonyl)-3,5-disubstituted-2,3-dihydro-1H-pyrazoles.

Authors:  M N Kumaraswamy; C Chandrashekhar; H Shivakumar; D A Prathima Mathias; K M Mahadevan; V P Vaidya
Journal:  Indian J Pharm Sci       Date:  2008-11       Impact factor: 0.975

8.  1-[3,5-Bis(4-chloro-phen-yl)-4,5-dihydro-1H-pyrazol-1-yl]ethanone.

Authors:  Jerry P Jasinski; Albert E Pek; S Samshuddin; B Narayana; H S Yathirajan
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-07-07

9.  3,5-Bis(4-fluoro-phen-yl)-4,5-dihydro-1H-pyrazole-1-carbaldehyde.

Authors:  Zeliha Baktır; Mehmet Akkurt; S Samshuddin; B Narayana; H S Yathirajan
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-05-07

10.  1-[5-(2H-1,3-Benzodioxol-5-yl)-3-(4-methyl-phen-yl)-2-pyrazolin-1-yl]ethanone.

Authors:  Wan-Sin Loh; Ibrahim Abdul Razak; M Abdul Rahiman; G N Ravikumar
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-04-13
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