Literature DB >> 10882007

New aromatase inhibitors. Synthesis and biological activity of aryl-substituted pyrrolizine and indolizine derivatives.

P Sonnet1, P Dallemagne, J Guillon, C Enguehard, S Stiebing, J Tanguy, R Bureau, S Rault, P Auvray, S Moslemi, P Sourdaine, G E Séralini.   

Abstract

We report herein the design and the synthesis of some aryl-substituted pyrrolizine and indolizine derivatives, on the basis of a hypothetical pharmacophore structure designed to fit the catalytic site of the human cytochrome P450 aromatase. The in vitro biological evaluation of these compounds allowed us to point out two new potent non-steroidal aromatase inhibitors, MR 20494 and MR 20492, with IC50 values in the range of 0.1 microM.

Entities:  

Mesh:

Substances:

Year:  2000        PMID: 10882007     DOI: 10.1016/s0968-0896(00)00024-9

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  10 in total

1.  Palladium(II)-catalyzed enantio- and diastereoselective synthesis of pyrrolidine derivatives.

Authors:  Ranjan Jana; Tejas P Pathak; Katrina H Jensen; Matthew S Sigman
Journal:  Org Lett       Date:  2012-08-08       Impact factor: 6.005

2.  (8aS)-7,8,8a,9-Tetra-hydro-thieno[3,2-f]indolizin-6(4H)-one.

Authors:  Lubomír Svorc; Viktor Vrábel; Jozef Kožíšek; Stefan Marchalín; Peter Safář
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2009-03-06

3.  (11R,11aS)-11-Hydr-oxy-1,5,11,11a-tetra-hydro-1-benzothieno[2,3-f]indolizin-3(2H)-one.

Authors:  Lubomír Svorc; Viktor Vrábel; Jozef Kožíšek; Stefan Marchalín; Peter Safář
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2008-05-30

4.  One-pot synthesis of 4-arylquinolines from aromatic aminoketones and vinylphosphonium salts.

Authors:  Sakineh Asghari; Mohammad Qandalee; Zahra Naderi; Zahra Sobhaninia
Journal:  Mol Divers       Date:  2009-08-13       Impact factor: 2.943

5.  Methyl 9-p-tolyl-8a,9,9a,10,11,12,13,14a-octa-hydro-8H-benzo[f]chromeno[3,4-b]indolizine-8a-carboxyl-ate.

Authors:  B Gunasekaran; S Kathiravan; R Raghunathan; V Manivannan
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2009-11-25

6.  (8aRS)-8,8a-Dihydro-furo[3,2-f]indolizine-6,9(4H,7H)-dione.

Authors:  Viktor Vrábel; Július Sivý; Lubomír Svorc; Peter Safář; Stefan Marchalín
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-07-13

7.  Enantioselective synthesis of polycyclic nitrogen heterocycles by Rh-catalyzed alkene hydroacylation: constructing six-membered rings in the absence of chelation assistance.

Authors:  Xiang-Wei Du; Avipsa Ghosh; Levi M Stanley
Journal:  Org Lett       Date:  2014-07-14       Impact factor: 6.005

8.  Microwave Assisted Reactions of Fluorescent Pyrrolodiazine Building Blocks.

Authors:  Costel Moldoveanu; Dorina Amariucai-Mantu; Violeta Mangalagiu; Vasilichia Antoci; Dan Maftei; Ionel I Mangalagiu; Gheorghita Zbancioc
Journal:  Molecules       Date:  2019-10-18       Impact factor: 4.411

9.  (5S,11aS)-5-Hydro-per-oxy-1,5,11,11a-tetra-hydro-[1]benzothieno[3,2-f]indol-izin-3(2H)-one.

Authors:  Viktor Vrábel; Lubomír Svorc; Stefan Marchalín; Peter Safář
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-11-10

10.  Huisgen [3 + 2] Dipolar Cycloadditions of Phthalazinium Ylides to Activated Symmetric and Non-Symmetric Alkynes.

Authors:  Vasilichia Antoci; Costel Moldoveanu; Ramona Danac; Violeta Mangalagiu; Gheorghita Zbancioc
Journal:  Molecules       Date:  2020-09-25       Impact factor: 4.411

  10 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.