An evaluation of Minor Groove Binders as anti-lung cancer therapeutics

Scott, Fraser J.; Puig-Sellart, Mireia; Khalaf, Abedawn I.; Henderson, Catherine; Westrop, Gareth D.; Watson, David; Carter, Katharine; Grant, M.H.; Suckling, Colin J.

doi:10.1016/j.bmcl.2016.06.040

Cited by 14 publications

(17 citation statements)

References 18 publications

(5 reference statements)

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“…This is a cell line derived from cells that metastasized to the lung and were isolated from lung metastatic nodules. 13 In that study, we identified that subtle structural variations significantly influenced the activity profile of the S-MGBs. Significantly, we were able to identify an S-MGB with around a 70-fold greater activity than gemcitabine, a current treatment option used in the clinic for non-small cell lung cancer.…”

Section: Introductionmentioning

confidence: 95%

Selective in vitro anti-cancer activity of non-alkylating minor groove binders

et al. 2019

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Section: Introductionmentioning

confidence: 95%

Selective in vitro anti-cancer activity of non-alkylating minor groove binders

et al. 2019

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“…Several focused reviews on small molecule DNA binding agents have been published in recent years. A few have updated the progresses made in disease specific DNA binders [ 14 – 15 ] while others have included class specific or site-specific DNA binding agents [ 16 – 23 ]. A few others have covered nucleic acids binders in general [ 20 ] as well as an emerging therapeutic DNA target: the DNA G-quadruplex [ 24 ].…”

Section: Reviewmentioning

confidence: 99%

“…Szerszenowicz et al developed a new set of potential minor groove binders derived from netropsin and bis-netropsin analogs by replacing N -methylpyrrole rings with other heterocyclic rings and their antiproliferative activity was tested on MCF-7 breast cancer cells [ 60 ]. Suckling et al recently designed and synthesized a series of structurally diverse MGBs, derived from distamycin, in order to test their lung cancer inhibition activity against the melanoma cancer cell line B16-F10 [ 14 ]. Conjugate 11 was found to be extremely potent and exhibits 70-fold activity in comparison to the standard therapy, gemcitabine.…”

Section: Reviewmentioning

confidence: 99%

An overview of recent advances in duplex DNA recognition by small molecules

Bhaduri

Ranjan

Arya

2018

Beilstein J. Org. Chem.

107

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As the carrier of genetic information, the DNA double helix interacts with many natural ligands during the cell cycle, and is amenable to such intervention in diseases such as cancer biogenesis. Proteins bind DNA in a site-specific manner, not only distinguishing between the geometry of the major and minor grooves, but also by making close contacts with individual bases within the local helix architecture. Over the last four decades, much research has been reported on the development of small non-natural ligands as therapeutics to either block, or in some cases, mimic a DNA–protein interaction of interest. This review presents the latest findings in the pursuit of novel synthetic DNA binders. This article provides recent coverage of major strategies (such as groove recognition, intercalation and cross-linking) adopted in the duplex DNA recognition by small molecules, with an emphasis on major works of the past few years.

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“…Distamycin does not possess significant cytotoxicity; however, other classes of minor groove binders have shown significant possibility as anti-cancer agents, in particular those which are derived from the distamycin structure (Scheme 9). 45 …”

Section: Mgbs For the Treatment Of Lung Cancermentioning

confidence: 99%

DNA Minor Groove Binders-Inspired by Nature

Khalaf¹,

Al-kadhimi²,

Ali³

2016

ACSi

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The synthesis and biological activity of a variety of analogues to the naturally occurring antibacterial and antifungal Distamycin A were explored by a number of authors. These compounds were subject to a large array of assays. Some of these compounds showed high activity against a range of Gram-positive, Gram-negative bacteria as well as fungi. To explore the anti-parasitic activity of this class of compounds, specific modifications had to be made. A number of these compounds proved to be active against Trypanosoma brucei. The binding of a number of these compounds to short sequences of DNA were also examined using footprinting assays as well as NMR spectroscopy. Computer modelling was employed on selected compounds to understand the way these compounds bind to specific DNA sequences. A large number of variations were made to the standard structure of Distamycin. These changes involved the replacement of the pyrrole moieties as well as the head and tail groups with a number of heterocyclic compounds. Some of these minor groove binders (MGBs) were also investigated for their capability for the treatment of cancer and in particular lung cancer.

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An evaluation of Minor Groove Binders as anti-lung cancer therapeutics

Cited by 14 publications

References 18 publications

Selective in vitro anti-cancer activity of non-alkylating minor groove binders

Selective in vitro anti-cancer activity of non-alkylating minor groove binders

An overview of recent advances in duplex DNA recognition by small molecules

DNA Minor Groove Binders-Inspired by Nature

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