Literature DB >> 29077404

Pharmacophore Hybridization To Discover Novel Topoisomerase II Poisons with Promising Antiproliferative Activity.

Jose Antonio Ortega1, Laura Riccardi1, Elirosa Minniti1,2, Marco Borgogno1, Jose M Arencibia1, Maria L Greco3, Anna Minarini2, Claudia Sissi3, Marco De Vivo1,4.   

Abstract

We used a pharmacophore hybridization strategy to combine key structural elements of merbarone and etoposide and generated new type II topoisomerase (topoII) poisons. This first set of hybrid topoII poisons shows promising antiproliferative activity on human cancer cells, endorsing their further exploration for anticancer drug discovery.

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Year:  2017        PMID： 29077404     DOI： 10.1021/acs.jmedchem.7b01388

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


  9 in total

Review 1.  Anticancer Profile of Rhodanines: Structure-Activity Relationship (SAR) and Molecular Targets-A Review.

Authors:  Jacek Szczepański; Helena Tuszewska; Nazar Trotsko
Journal:  Molecules       Date:  2022-06-10       Impact factor: 4.927

2.  Polyamine-containing etoposide derivatives as poisons of human type II topoisomerases: Differential effects on topoisomerase IIα and IIβ.

Authors:  Alexandria A Oviatt; Jissy A Kuriappan; Elirosa Minniti; Kendra R Vann; Princess Onuorah; Anna Minarini; Marco De Vivo; Neil Osheroff
Journal:  Bioorg Med Chem Lett       Date:  2018-07-05       Impact factor: 2.823

3.  Synthesis and antitumor activity of fluorouracil - oleanolic acid/ursolic acid/glycyrrhetinic acid conjugates.

Authors:  Chun-Mei Liu; Jia-Yan Huang; Li-Xin Sheng; Xiao-An Wen; Ke-Guang Cheng
Journal:  Medchemcomm       Date:  2019-06-12       Impact factor: 3.597

4.  Design, synthesis and biological evaluation of benzimidazole-rhodanine conjugates as potent topoisomerase II inhibitors.

Authors:  Penghui Li; Wenjin Zhang; Hong Jiang; Yongliang Li; Changzhi Dong; Huixiong Chen; Kun Zhang; Zhiyun Du
Journal:  Medchemcomm       Date:  2018-06-02       Impact factor: 3.597

5.  Novel Bacterial Topoisomerase Inhibitors Exploit Asp83 and the Intrinsic Flexibility of the DNA Gyrase Binding Site.

Authors:  Sebastian Franco-Ulloa; Giuseppina La Sala; Gian Pietro Miscione; Marco De Vivo
Journal:  Int J Mol Sci       Date:  2018-02-03       Impact factor: 5.923

6.  Design, Synthesis and Anti-Tumor Activity of Novel Benzimidazole-Chalcone Hybrids as Non-Intercalative Topoisomerase II Catalytic Inhibitors.

Authors:  Wei Zhou; Wenjin Zhang; Yi Peng; Zhi-Hong Jiang; Lanyue Zhang; Zhiyun Du
Journal:  Molecules       Date:  2020-07-12       Impact factor: 4.411

7.  Smoothed Potential MD Simulations for Dissociation Kinetics of Etoposide To Unravel Isoform Specificity in Targeting Human Topoisomerase II.

Authors:  Jissy A Kuriappan; Neil Osheroff; Marco De Vivo
Journal:  J Chem Inf Model       Date:  2019-09-09       Impact factor: 4.956

8.  Novel, Potent, and Druglike Tetrahydroquinazoline Inhibitor That Is Highly Selective for Human Topoisomerase II α over β.

Authors:  Jose Antonio Ortega; Jose M Arencibia; Elirosa Minniti; Jo Ann W Byl; Sebastian Franco-Ulloa; Marco Borgogno; Vito Genna; Maria Summa; Sine Mandrup Bertozzi; Rosalia Bertorelli; Andrea Armirotti; Anna Minarini; Claudia Sissi; Neil Osheroff; Marco De Vivo
Journal:  J Med Chem       Date:  2020-10-20       Impact factor: 7.446

9.  Design and synthesis of thiadiazolo-carboxamide bridged β-carboline-indole hybrids: DNA intercalative topo-IIα inhibition with promising antiproliferative activity.

Authors:  Ramya Tokala; Sravani Sana; Uppu Jaya Lakshmi; Prasanthi Sankarana; Dilep Kumar Sigalapalli; Nikhil Gadewal; Jyoti Kode; Nagula Shankaraiah
Journal:  Bioorg Chem       Date:  2020-10-08       Impact factor: 5.275
  9 in total

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