Literature DB >> 11728195

Design, synthesis, and biological activity of a novel non-cisplatin-type platinum-acridine pharmacophore.

E T Martins1, H Baruah, J Kramarczyk, G Saluta, C S Day, G L Kucera, U Bierbach.   

Abstract

Platinum-acridine conjugates were prepared from [PtCl2(ethane-1,2-diamine)] and the novel acridinylthioureas MeHNC(S)NMeAcr (6) and MeHNC(S)NMe(CH2CH2)NHAcr (15) by replacing one chloro leaving group in the cisplatin analogue with thiourea sulfur. In HL-60 leukemia cells, IC(50) values for 7 (Pt-tethered 6) and 16 (Pt-tethered 15) were 75 and 0.13 microM, respectively. In the ovarian cell lines 2008 and C13, 16 was active at micromolar concentrations and showed only partial cross-resistance with clinical cisplatin. Possible structure-activity relationships are discussed.

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Year:  2001        PMID： 11728195     DOI： 10.1021/jm010293m

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  29 in total

1.  Unusual intercalation of acridin-9-ylthiourea into the 5'-GA/TC DNA base step from the minor groove: implications for the covalent DNA adduct profile of a novel platinum-intercalator conjugate.

Authors:  Hemanta Baruah; Ulrich Bierbach
Journal:  Nucleic Acids Res       Date:  2003-07-15       Impact factor: 16.971

Review 2.  Synthetic methods for the preparation of platinum anticancer complexes.

Authors:  Justin J Wilson; Stephen J Lippard
Journal:  Chem Rev       Date:  2013-11-27       Impact factor: 60.622

3.  Replacement of a thiourea with an amidine group in a monofunctional platinum-acridine antitumor agent. Effect on DNA interactions, DNA adduct recognition and repair.

Authors:  Hana Kostrhunova; Jaroslav Malina; Amanda J Pickard; Jana Stepankova; Marie Vojtiskova; Jana Kasparkova; Tereza Muchova; Matthew L Rohlfing; Ulrich Bierbach; Viktor Brabec
Journal:  Mol Pharm       Date:  2011-08-17       Impact factor: 4.939

4.  Human Serum Albumin-Delivered [Au(PEt3)]+ Is a Potent Inhibitor of T Cell Proliferation.

Authors:  Tyler C Dean; Mu Yang; Mingyong Liu; Jason M Grayson; Anthony W DeMartino; Cynthia S Day; Jingyun Lee; Cristina M Furdui; Ulrich Bierbach
Journal:  ACS Med Chem Lett       Date:  2017-04-25       Impact factor: 4.345

5.  Comparative chemogenomics to examine the mechanism of action of dna-targeted platinum-acridine anticancer agents.

Authors:  Kahlin Cheung-Ong; Kyung Tae Song; Zhidong Ma; Daniel Shabtai; Anna Y Lee; David Gallo; Lawrence E Heisler; Grant W Brown; Ulrich Bierbach; Guri Giaever; Corey Nislow
Journal:  ACS Chem Biol       Date:  2012-09-05       Impact factor: 5.100

6.  Synthesis, aqueous reactivity, and biological evaluation of carboxylic acid ester-functionalized platinum-acridine hybrid anticancer agents.

Authors:  Leigh A Graham; Jimmy Suryadi; Tiffany K West; Gregory L Kucera; Ulrich Bierbach
Journal:  J Med Chem       Date:  2012-08-17       Impact factor: 7.446

7.  Unusual Reactivity of a Potent Platinum-Acridine Hybrid Antitumor Agent.

Authors:  Leigh A Graham; Gary M Wilson; Tiffany K West; Cynthia S Day; Gregory L Kucera; Ulrich Bierbach
Journal:  ACS Med Chem Lett       Date:  2011-09-08       Impact factor: 4.345

Review 8.  The Next Generation of Platinum Drugs: Targeted Pt(II) Agents, Nanoparticle Delivery, and Pt(IV) Prodrugs.

Authors:  Timothy C Johnstone; Kogularamanan Suntharalingam; Stephen J Lippard
Journal:  Chem Rev       Date:  2016-02-11       Impact factor: 60.622

9.  Replacement of a thiourea-S with an amidine-NH donor group in a platinum-acridine antitumor compound reduces the metal's reactivity with cysteine sulfur.

Authors:  Zhidong Ma; Lu Rao; Ulrich Bierbach
Journal:  J Med Chem       Date:  2009-05-28       Impact factor: 7.446

10.  Synthesis and biological evaluation of platinum-acridine hybrid agents modified with bipyridine non-leaving groups.

Authors:  Alexander R Kheradi; Gilda Saluta; Gregory L Kucera; Cynthia S Day; Ulrich Bierbach
Journal:  Bioorg Med Chem Lett       Date:  2009-05-18       Impact factor: 2.823
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