Literature DB >> 19875282

Isoquinoline-based analogs of the cancer drug clinical candidate tipifarnib as anti-Trypanosoma cruzi agents.

Naveen Kumar Chennamaneni1, Jenifer Arif, Frederick S Buckner, Michael H Gelb.   

Abstract

We developed a synthetic route to prepare isoquinoline analogs of the cancer drug clinical candidate tipifarnib. We show that these compounds kill Trypanosoma cruzi amastigotes grown in mammalian host cells at concentrations in the low nanomolar range. These isoquinolines represent new leads for the development of drugs to treat Chagas disease.

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Year:  2009        PMID： 19875282      PMCID： PMC2783978          DOI： 10.1016/j.bmcl.2009.10.029

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


  4 in total

1.  Efficient technique for screening drugs for activity against Trypanosoma cruzi using parasites expressing beta-galactosidase.

Authors:  F S Buckner; C L Verlinde; A C La Flamme; W C Van Voorhis
Journal:  Antimicrob Agents Chemother       Date:  1996-11       Impact factor: 5.191

2.  Rational modification of a candidate cancer drug for use against Chagas disease.

Authors:  James M Kraus; Christophe L M J Verlinde; Mandana Karimi; Galina I Lepesheva; Michael H Gelb; Frederick S Buckner
Journal:  J Med Chem       Date:  2009-03-26       Impact factor: 7.446

3.  The protein farnesyltransferase inhibitor Tipifarnib as a new lead for the development of drugs against Chagas disease.

Authors:  Oliver Hucke; Michael H Gelb; Christophe L M J Verlinde; Frederick S Buckner
Journal:  J Med Chem       Date:  2005-08-25       Impact factor: 7.446

4.  Cure of short- and long-term experimental Chagas' disease using D0870.

Authors:  J A Urbina; G Payares; J Molina; C Sanoja; A Liendo; K Lazardi; M M Piras; R Piras; N Perez; P Wincker; J F Ryley
Journal:  Science       Date:  1996-08-16       Impact factor: 47.728
  4 in total
  10 in total

1.  Structural characterization of CYP51 from Trypanosoma cruzi and Trypanosoma brucei bound to the antifungal drugs posaconazole and fluconazole.

Authors:  Chiung-Kuang Chen; Siegfried S F Leung; Christophe Guilbert; Matthew P Jacobson; James H McKerrow; Larissa M Podust
Journal:  PLoS Negl Trop Dis       Date:  2010-04-06

2.  Crystal Structure and Hirshfeld Surface Analysis of Acetoacetanilide Based Reaction Products.

Authors:  Farid N Naghiyev; Jonathan Cisterna; Ali N Khalilov; Abel M Maharramov; Rizvan K Askerov; Khammed A Asadov; Ibrahim G Mamedov; Khaver S Salmanli; Alejandro Cárdenas; Ivan Brito
Journal:  Molecules       Date:  2020-05-09       Impact factor: 4.411

Review 3.  Trypanocidal activity of marine natural products.

Authors:  Amy J Jones; Tanja Grkovic; Melissa L Sykes; Vicky M Avery
Journal:  Mar Drugs       Date:  2013-10-22       Impact factor: 5.118

Review 4.  Drug strategies targeting CYP51 in neglected tropical diseases.

Authors:  Jun Yong Choi; Larissa M Podust; William R Roush
Journal:  Chem Rev       Date:  2014-10-22       Impact factor: 60.622

5.  Binding mode and potency of N-indolyloxopyridinyl-4-aminopropanyl-based inhibitors targeting Trypanosoma cruzi CYP51.

Authors:  Debora F Vieira; Jun Yong Choi; Claudia M Calvet; Jair Lage Siqueira-Neto; Jonathan B Johnston; Danielle Kellar; Jiri Gut; Michael D Cameron; James H McKerrow; William R Roush; Larissa M Podust
Journal:  J Med Chem       Date:  2014-11-25       Impact factor: 7.446

6.  Chemical-biological characterization of a cruzain inhibitor reveals a second target and a mammalian off-target.

Authors:  Jonathan W Choy; Clifford Bryant; Claudia M Calvet; Patricia S Doyle; Shamila S Gunatilleke; Siegfried S F Leung; Kenny K H Ang; Steven Chen; Jiri Gut; Juan A Oses-Prieto; Jonathan B Johnston; Michelle R Arkin; Alma L Burlingame; Jack Taunton; Matthew P Jacobson; James M McKerrow; Larissa M Podust; Adam R Renslo
Journal:  Beilstein J Org Chem       Date:  2013-01-04       Impact factor: 2.883

7.  Diverse inhibitor chemotypes targeting Trypanosoma cruzi CYP51.

Authors:  Shamila S Gunatilleke; Claudia M Calvet; Jonathan B Johnston; Chiung-Kuang Chen; Grigori Erenburg; Jiri Gut; Juan C Engel; Kenny K H Ang; Joseph Mulvaney; Steven Chen; Michelle R Arkin; James H McKerrow; Larissa M Podust
Journal:  PLoS Negl Trop Dis       Date:  2012-07-31

8.  4-Aminopyridyl-based CYP51 inhibitors as anti-Trypanosoma cruzi drug leads with improved pharmacokinetic profile and in vivo potency.

Authors:  Claudia M Calvet; Debora F Vieira; Jun Yong Choi; Danielle Kellar; Michael D Cameron; Jair Lage Siqueira-Neto; Jiri Gut; Jonathan B Johnston; Li Lin; Susan Khan; James H McKerrow; William R Roush; Larissa M Podust
Journal:  J Med Chem       Date:  2014-08-19       Impact factor: 7.446

Review 9.  Synthetic Medicinal Chemistry in Chagas' Disease: Compounds at The Final Stage of "Hit-To-Lead" Phase.

Authors:  Hugo Cerecetto; Mercedes González
Journal:  Pharmaceuticals (Basel)       Date:  2010-03-25

10.  N-Substituted Auxiliaries for Aerobic Dehydrogenation of Tetrahydro-isoquinoline: A Theory-Guided Photo-Catalytic Design.

Authors:  Savithra Jayaraj; Abraham K Badu-Tawiah
Journal:  Sci Rep       Date:  2019-08-02       Impact factor: 4.379
  10 in total

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