Literature DB >> 10498189

Human telomerase inhibition by substituted acridine derivatives.

R J Harrison1, S M Gowan, L R Kelland, S Neidle.   

Abstract

A series of 3,6-disubstituted acridine derivatives have been rationally designed as telomerase inhibitors. They have been designed on the basis that inhibition of telomerase occurs by stabilising G-quadruplex structures formed by the folding of telomeric DNA. The most potent inhibitors have IC50 values against telomerase of between 1.3 and 8 microM, comparable to their cytotoxicity in ovarian cancer cell lines.

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Year:  1999        PMID: 10498189     DOI: 10.1016/s0960-894x(99)00394-7

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


  19 in total

Review 1.  Tiptoeing to chromosome tips: facts, promises and perils of today's human telomere biology.

Authors:  J Fajkus; M Simícková; J Maláska
Journal:  Philos Trans R Soc Lond B Biol Sci       Date:  2002-04-29       Impact factor: 6.237

2.  Rational design of substituted diarylureas: a scaffold for binding to G-quadruplex motifs.

Authors:  William C Drewe; Rupesh Nanjunda; Mekala Gunaratnam; Monica Beltran; Gary N Parkinson; Anthony P Reszka; W David Wilson; Stephen Neidle
Journal:  J Med Chem       Date:  2008-12-25       Impact factor: 7.446

3.  Targeting human telomerase for cancer therapeutics.

Authors:  Lionel Guittat; Patrizia Alberti; Dennis Gomez; Anne De Cian; Gaëlle Pennarun; Thibault Lemarteleur; Chafke Belmokhtar; Rajaa Paterski; Hamid Morjani; Chantal Trentesaux; Eliane Mandine; François Boussin; Patrick Mailliet; Laurent Lacroix; Jean-François Riou; Jean-Louis Mergny
Journal:  Cytotechnology       Date:  2004-06       Impact factor: 2.058

4.  Molecular dynamics and principal components analysis of human telomeric quadruplex multimers.

Authors:  Shozeb Haider; Gary N Parkinson; Stephen Neidle
Journal:  Biophys J       Date:  2008-03-28       Impact factor: 4.033

5.  Structure-based design of selective and potent G quadruplex-mediated telomerase inhibitors.

Authors:  M Read; R J Harrison; B Romagnoli; F A Tanious; S H Gowan; A P Reszka; W D Wilson; L R Kelland; S Neidle
Journal:  Proc Natl Acad Sci U S A       Date:  2001-04-17       Impact factor: 11.205

6.  Macrocyclic pyridyl polyoxazoles: selective RNA and DNA G-quadruplex ligands as antitumor agents.

Authors:  Suzanne G Rzuczek; Daniel S Pilch; Angela Liu; Leroy Liu; Edmond J LaVoie; Joseph E Rice
Journal:  J Med Chem       Date:  2010-05-13       Impact factor: 7.446

7.  Exploiting σ-hole interaction to design small uncharged ligand molecules to stabilize G-quadruplex-DNA: a computational study.

Authors:  Mrinal Kanti Si; Anusuya Saha; Bishwajit Ganguly
Journal:  J Mol Model       Date:  2020-02-01       Impact factor: 1.810

8.  Recognition and discrimination of DNA quadruplexes by acridine-peptide conjugates.

Authors:  James E Redman; J M Granadino-Roldán; James A Schouten; Sylvain Ladame; Anthony P Reszka; Stephen Neidle; Shankar Balasubramanian
Journal:  Org Biomol Chem       Date:  2008-10-30       Impact factor: 3.876

9.  Telomere maintenance in childhood primitive neuroectodermal brain tumors.

Authors:  Domenico Didiano; Tarek Shalaby; Doris Lang; Michael A Grotzer
Journal:  Neuro Oncol       Date:  2004-01       Impact factor: 12.300

Review 10.  Structure-based DNA-targeting strategies with small molecule ligands for drug discovery.

Authors:  Jia Sheng; Jianhua Gan; Zhen Huang
Journal:  Med Res Rev       Date:  2013-04-30       Impact factor: 12.944

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