Literature DB >> 30104277

Activity of Aromathecins against African Trypanosomes.

Nathaniel P Nenortas1, Maris A Cinelli2, Andrew E Morrell2, Mark Cushman2, Theresa A Shapiro3.   

Abstract

African sleeping sickness is responsible for thousands of deaths annually, and new therapeutics are needed. This study evaluated aromathecins, experimental inhibitors of mammalian topoisomerase IB, against Trypanosoma brucei African trypanosomes. The compounds had selectively toxic antiparasitic potency, in situ poisoning activity against the phylogenetically unique topoisomerase in these parasites, and a representative compound intercalated into DNA with micromolar affinity. DNA intercalation and topoisomerase poisoning may contribute to the antitrypanosomal activity of aromathecins.
Copyright © 2018 American Society for Microbiology.

Entities:  

Keywords:  Trypanosoma brucei; aromathecin; sleeping sickness; structure-activity; topoisomerase

Mesh：

Substances：

Year:  2018        PMID： 30104277      PMCID： PMC6201061          DOI： 10.1128/AAC.00786-18

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN： 0066-4804            Impact factor:   5.191


  21 in total

1.  A model for the mechanism of human topoisomerase I.

Authors:  L Stewart; M R Redinbo; X Qiu; W G Hol; J J Champoux
Journal:  Science       Date:  1998-03-06       Impact factor: 47.728

2.  Synthesis and evaluation of indenoisoquinoline topoisomerase I inhibitors substituted with nitrogen heterocycles.

Authors:  Muthukaman Nagarajan; Andrew Morrell; Alexandra Ioanoviciu; Smitha Antony; Glenda Kohlhagen; Keli Agama; Melinda Hollingshead; Yves Pommier; Mark Cushman
Journal:  J Med Chem       Date:  2006-10-19       Impact factor: 7.446

3.  Newly identified antibacterial compounds are topoisomerase poisons in African trypanosomes.

Authors:  Sonya C Tang; Theresa A Shapiro
Journal:  Antimicrob Agents Chemother       Date:  2009-12-14       Impact factor: 5.191

4.  Synthesis and biological evaluation of 14-(aminoalkyl-aminomethyl)aromathecins as topoisomerase I inhibitors: investigating the hypothesis of shared structure-activity relationships.

Authors:  Maris A Cinelli; Brenda Cordero; Thomas S Dexheimer; Yves Pommier; Mark Cushman
Journal:  Bioorg Med Chem       Date:  2009-09-06       Impact factor: 3.641

5.  Oral fexinidazole for late-stage African Trypanosoma brucei gambiense trypanosomiasis: a pivotal multicentre, randomised, non-inferiority trial.

Authors:  Victor Kande Betu Ku Mesu; Wilfried Mutombo Kalonji; Clélia Bardonneau; Olaf Valverde Mordt; Séverine Blesson; François Simon; Sophie Delhomme; Sonja Bernhard; Willy Kuziena; Jean-Pierre Fina Lubaki; Steven Lumeya Vuvu; Pathou Nganzobo Ngima; Hélène Mahenzi Mbembo; Médard Ilunga; Augustin Kasongo Bonama; Josué Amici Heradi; Jean Louis Lumaliza Solomo; Guylain Mandula; Lewis Kaninda Badibabi; Francis Regongbenga Dama; Papy Kavunga Lukula; Digas Ngolo Tete; Crispin Lumbala; Bruno Scherrer; Nathalie Strub-Wourgaft; Antoine Tarral
Journal:  Lancet       Date:  2017-11-04       Impact factor: 79.321

6.  Antitrypanosomal activity of camptothecin analogs. Structure-activity correlations.

Authors:  A L Bodley; M C Wani; M E Wall; T A Shapiro
Journal:  Biochem Pharmacol       Date:  1995-09-28       Impact factor: 5.858

7.  An unusual type IB topoisomerase from African trypanosomes.

Authors:  Annette L Bodley; Asit K Chakraborty; Suji Xie; Christian Burri; Theresa A Shapiro
Journal:  Proc Natl Acad Sci U S A       Date:  2003-06-16       Impact factor: 11.205

8.  Molecular and cytotoxic effects of camptothecin, a topoisomerase I inhibitor, on trypanosomes and Leishmania.

Authors:  A L Bodley; T A Shapiro
Journal:  Proc Natl Acad Sci U S A       Date:  1995-04-25       Impact factor: 11.205

Review 9.  Anti-trypanosomatid drug discovery: an ongoing challenge and a continuing need.

Authors:  Mark C Field; David Horn; Alan H Fairlamb; Michael A J Ferguson; David W Gray; Kevin D Read; Manu De Rycker; Leah S Torrie; Paul G Wyatt; Susan Wyllie; Ian H Gilbert
Journal:  Nat Rev Microbiol       Date:  2017-02-27       Impact factor: 60.633

10.  Determination of an optimal dosing regimen for fexinidazole, a novel oral drug for the treatment of human African trypanosomiasis: first-in-human studies.

Authors:  Antoine Tarral; Séverine Blesson; Olaf Valverde Mordt; Els Torreele; Daniela Sassella; Michael A Bray; Lionel Hovsepian; Eric Evène; Virginie Gualano; Mathieu Felices; Nathalie Strub-Wourgaft
Journal:  Clin Pharmacokinet       Date:  2014-06       Impact factor: 6.447
View more
  2 in total

1.  Antiparasitic effect of synthetic aromathecins on Leishmania infantum.

Authors:  Rosa M Reguera; Raquel Álvarez-Velilla; Bárbara Domínguez-Asenjo; Camino Gutiérrez-Corbo; Rafael Balaña-Fouce; Mark Cushman; Yolanda Pérez-Pertejo
Journal:  BMC Vet Res       Date:  2019-11-09       Impact factor: 2.741

2.  Transannular Approach to 2,3-Dihydropyrrolo[1,2-b]isoquinolin-5(1H)-ones through Brønsted Acid-Catalyzed Amidohalogenation.

Authors:  Estefanía Capel; Javier Luis-Barrera; Ana Sorazu; Uxue Uria; Liher Prieto; Efraím Reyes; Luisa Carrillo; Jose L Vicario
Journal:  J Org Chem       Date:  2022-07-26       Impact factor: 4.198
  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.