Literature DB >> 28835791

Synthesis and Activity of a New Series of Antileishmanial Agents.

Ankush Kanwar1, Benjamin J Eduful1, Linda Barbeto1, Piero Carletti Bonomo1, Andrea Lemus1, Brian A Vesely2, Tina S Mutka2, Ala Azhari2, Dennis E Kyle2, James W Leahy1,3,4.   

Abstract

We have determined that tetrahydroindazoles such as 1 show potent activity against Leishmania donovani, the causative agent of leishmaniasis. While the Hsp90 activity and anticancer properties of 1 have previously been explored, we present here our efforts to optimize their activity against L. donovani via the synthesis of novel analogues designed to probe the hydrophobic pocket of the protozoan Hsp90 orthologue, specifically through the auspices of functionalization of an amine embedded into the scaffold.

Entities:  

Keywords:  Antiinfectives; Hsp90; chaperone; leishmaniasis

Year:  2017        PMID： 28835791      PMCID： PMC5554902          DOI： 10.1021/acsmedchemlett.7b00039

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.632


  24 in total

1.  Targeting of the protein chaperone, HSP90, by the transformation suppressing agent, radicicol.

Authors:  S V Sharma; T Agatsuma; H Nakano
Journal:  Oncogene       Date:  1998-05       Impact factor: 9.867

2.  Phase I dose-escalation studies of SNX-5422, an orally bioavailable heat shock protein 90 inhibitor, in patients with refractory solid tumours.

Authors:  Jeffrey R Infante; Glen J Weiss; Suzanne Jones; Raoul Tibes; Todd M Bauer; Johanna C Bendell; James M Hinson; Daniel D Von Hoff; Howard A Burris; Everardus O Orlemans; Ramesh K Ramanathan
Journal:  Eur J Cancer       Date:  2014-09-25       Impact factor: 9.162

3.  The claisen rearrangement in indole alkaloid synthesis. The total synthesis of ( )-tabersonine.

Authors:  F E Ziegler; G B Bennett
Journal:  J Am Chem Soc       Date:  1973-10-31       Impact factor: 15.419

Review 4.  Targeting the dynamic HSP90 complex in cancer.

Authors:  Jane Trepel; Mehdi Mollapour; Giuseppe Giaccone; Len Neckers
Journal:  Nat Rev Cancer       Date:  2010-08       Impact factor: 60.716

5.  Exploring in vitro and in vivo Hsp90 inhibitors activity against human protozoan parasites.

Authors:  Giuseppe Giannini; Gianfranco Battistuzzi
Journal:  Bioorg Med Chem Lett       Date:  2014-12-20       Impact factor: 2.823

Review 6.  Leishmaniasis: current situation and new perspectives.

Authors:  P Desjeux
Journal:  Comp Immunol Microbiol Infect Dis       Date:  2004-09       Impact factor: 2.268

7.  Potent antitrypanosomal activities of heat shock protein 90 inhibitors in vitro and in vivo.

Authors:  Kirsten J Meyer; Theresa A Shapiro
Journal:  J Infect Dis       Date:  2013-04-22       Impact factor: 5.226

8.  Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents.

Authors:  Kenneth H Huang; James M Veal; R Patrick Fadden; John W Rice; Jeron Eaves; Jon-Paul Strachan; Amy F Barabasz; Briana E Foley; Thomas E Barta; Wei Ma; Melanie A Silinski; Mei Hu; Jeffrey M Partridge; Anisa Scott; Laura G DuBois; Tiffany Freed; Paul M Steed; Andy J Ommen; Emilie D Smith; Philip F Hughes; Angela R Woodward; Gunnar J Hanson; W Stephen McCall; Christopher J Markworth; Lindsay Hinkley; Matthew Jenks; Lifeng Geng; Meredith Lewis; James Otto; Bert Pronk; Katleen Verleysen; Steven E Hall
Journal:  J Med Chem       Date:  2009-07-23       Impact factor: 7.446

Review 9.  Targeting Hsp90 in Non-Cancerous Maladies.

Authors:  Mark R Woodford; Diana M Dunn; Joseph G Ciciarelli; Kristin Beebe; Len Neckers; Mehdi Mollapour
Journal:  Curr Top Med Chem       Date:  2016       Impact factor: 3.295

10.  Development of a fluorescence polarization assay for the molecular chaperone Hsp90.

Authors:  Joungnam Kim; Sara Felts; Laura Llauger; Huazhong He; Henri Huezo; Neal Rosen; Gabriela Chiosis
Journal:  J Biomol Screen       Date:  2004-08
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  1 in total

1.  A docking-based structural analysis of geldanamycin-derived inhibitor binding to human or Leishmania Hsp90.

Authors:  Luana Carneiro Palma; Luiz Felipe Gomes Rebello Ferreira; Antonio Luis de Oliveira Almeida Petersen; Beatriz Rocha Simões Dias; Juliana Perrone Bezerra de Menezes; Diogo Rodrigo de Magalhães Moreira; Marcelo Zaldini Hernandes; Patricia Sampaio Tavares Veras
Journal:  Sci Rep       Date:  2019-10-14       Impact factor: 4.379
  1 in total

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