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Items: 1 to 20 of 104


Synthesis of marine α-methoxylated fatty acid analogs that effectively inhibit the topoisomerase IB from Leishmania donovani with a mechanism different from that of camptothecin.

Carballeira NM, Montano N, Alvarez-Velilla R, Prada CF, Reguera RM, Balaña-Fouce R.

Mar Drugs. 2013 Sep 30;11(10):3661-75. doi: 10.3390/md11103661.


2-Alkynoic fatty acids inhibit topoisomerase IB from Leishmania donovani.

Carballeira NM, Cartagena M, Sanabria D, Tasdemir D, Prada CF, Reguera RM, Balaña-Fouce R.

Bioorg Med Chem Lett. 2012 Oct 1;22(19):6185-9. doi: 10.1016/j.bmcl.2012.08.019. Epub 2012 Aug 10.


Novel Very Long-Chain α-Methoxylated Δ5,9 Fatty Acids from the Sponge Asteropus niger Are Effective Inhibitors of Topoisomerases IB.

Carballeira NM, Montano N, Amador LA, Rodríguez AD, Golovko MY, Golovko SA, Reguera RM, Álvarez-Velilla R, Balaña-Fouce R.

Lipids. 2016 Feb;51(2):245-56. doi: 10.1007/s11745-015-4114-9. Epub 2015 Dec 22.


A Novel Spirooxindole Derivative Inhibits the Growth of Leishmania donovani Parasites both In Vitro and In Vivo by Targeting Type IB Topoisomerase.

Saha S, Acharya C, Pal U, Chowdhury SR, Sarkar K, Maiti NC, Jaisankar P, Majumder HK.

Antimicrob Agents Chemother. 2016 Sep 23;60(10):6281-93. doi: 10.1128/AAC.00352-16. Print 2016 Oct.


The lignan glycosides lyoniside and saracoside poison the unusual type IB topoisomerase of Leishmania donovani and kill the parasite both in vitro and in vivo.

Saha S, Mukherjee T, Chowdhury S, Mishra A, Chowdhury SR, Jaisankar P, Mukhopadhyay S, Majumder HK.

Biochem Pharmacol. 2013 Dec 15;86(12):1673-87. doi: 10.1016/j.bcp.2013.10.004. Epub 2013 Oct 14.


Total synthesis and antileishmanial activity of the natural occurring acetylenic fatty acids 6-heptadecynoic acid and 6-icosynoic acid.

Carballeira NM, Cartagena MM, Prada CF, Rubio CF, Balaña-Fouce R.

Lipids. 2009 Oct;44(10):953-61. doi: 10.1007/s11745-009-3345-z. Epub 2009 Sep 30.


First total synthesis of the (±)-2-methoxy-6-heptadecynoic acid and related 2-methoxylated analogs as effective inhibitors of the leishmania topoisomerase IB enzyme.

Carballeira NM, Cartagena M, Li F, Chen Z, Prada CF, Calvo-Alvarez E, Reguera RM, Balaña-Fouce R.

Pure Appl Chem. 2012;84(9):1867-1875. Epub 2012 Apr 29.


Antileishmanial activity evaluation of bis-lawsone analogs and DNA topoisomerase-I inhibition studies.

Sharma G, Chowdhury S, Sinha S, Majumder HK, Kumar SV.

J Enzyme Inhib Med Chem. 2014 Apr;29(2):185-9. doi: 10.3109/14756366.2013.765413. Epub 2013 Mar 27.


Recent developments in the antiprotozoal and anticancer activities of the 2-alkynoic fatty acids.

Carballeira NM.

Chem Phys Lipids. 2013 Jul-Aug;172-173:58-66. doi: 10.1016/j.chemphyslip.2013.05.002. Epub 2013 May 28. Review.


Gimatecan and other camptothecin derivatives poison Leishmania DNA-topoisomerase IB leading to a strong leishmanicidal effect.

Prada CF, Alvarez-Velilla R, Balaña-Fouce R, Prieto C, Calvo-Álvarez E, Escudero-Martínez JM, Requena JM, Ordóñez C, Desideri A, Pérez-Pertejo Y, Reguera RM.

Biochem Pharmacol. 2013 May 15;85(10):1433-40. doi: 10.1016/j.bcp.2013.02.024. Epub 2013 Mar 1.


The facile synthesis of the 5Z,9Z-dienoic acids and their topoisomerase I inhibitory activity.

D'yakonov VA, Makarov AA, Dzhemileva LU, Makarova EKh, Khusnutdinova EK, Dzhemilev UM.

Chem Commun (Camb). 2013 Sep 28;49(75):8401-3. doi: 10.1039/c3cc44926b.


First total synthesis and antiprotozoal activity of (Z)-17-methyl-13-octadecenoic acid, a new marine fatty acid from the sponge Polymastia penicillus.

Carballeira NM, Montano N, Balaña-Fouce R, Prada CF.

Chem Phys Lipids. 2009 Sep;161(1):38-43. doi: 10.1016/j.chemphyslip.2009.06.140. Epub 2009 Jun 13.


A pentapeptide signature motif plays a pivotal role in Leishmania DNA topoisomerase IB activity and camptothecin sensitivity.

Prada CF, Alvarez-Velilla R, Diaz-González R, Prieto C, Pérez-Pertejo Y, Balaña-Fouce R, Reguera RM.

Biochim Biophys Acta. 2012 Dec;1820(12):2062-71. doi: 10.1016/j.bbagen.2012.09.005. Epub 2012 Sep 18.


A new bisbenzylisoquinoline alkaloid isolated from Thalictrum foliolosum, as a potent inhibitor of DNA topoisomerase IB of Leishmania donovani.

Kumar A, Chowdhury SR, Sarkar T, Chakrabarti T, Majumder HK, Jha T, Mukhopadhyay S.

Fitoterapia. 2016 Mar;109:25-30. doi: 10.1016/j.fitote.2015.11.021. Epub 2015 Nov 26.


First total synthesis and antileishmanial activity of (Z)-16-methyl-11-heptadecenoic acid, a new marine fatty acid from the sponge Dragmaxia undata.

Carballeira NM, Montano N, Cintrón GA, Márquez C, Rubio CF, Prada CF, Balaña-Fouce R.

Chem Phys Lipids. 2011 Feb;164(2):113-7. doi: 10.1016/j.chemphyslip.2010.11.006. Epub 2010 Dec 1.


Mutational study of the "catalytic tetrad" of DNA topoisomerase IB from the hemoflagellate Leishmania donovani: Role of Asp-353 and Asn-221 in camptothecin resistance.

Diaz-González R, Pérez-Pertejo Y, Pommier Y, Balaña-Fouce R, Reguera RM.

Biochem Pharmacol. 2008 Sep 1;76(5):608-19. doi: 10.1016/j.bcp.2008.06.019. Epub 2008 Jul 4.


Voacamine alters Leishmania ultrastructure and kills parasite by poisoning unusual bi-subunit topoisomerase IB.

Chowdhury SR, Kumar A, Godinho JLP, De Macedo Silva ST, Zuma AA, Saha S, Kumari N, Rodrigues JCF, Sundar S, Dujardin JC, Roy S, De Souza W, Mukhopadhyay S, Majumder HK.

Biochem Pharmacol. 2017 Aug 15;138:19-30. doi: 10.1016/j.bcp.2017.05.002. Epub 2017 May 5.


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