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Sequence selective pyrrole and imidazole polyamide metallocomplexes

A technology for imidazole polyamides and complexes, which is applied in the directions of active ingredients of heterocyclic compounds, drug combinations, organic active ingredients, etc., can solve the problem of lack of sequence selectivity and the like

Inactive Publication Date: 2006-11-15
UNIVERSITY OF WESTERN SYDNEY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, despite its affinity for sequences in the minor groove, distal mycin is not sequence selective

Method used

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  • Sequence selective pyrrole and imidazole polyamide metallocomplexes
  • Sequence selective pyrrole and imidazole polyamide metallocomplexes
  • Sequence selective pyrrole and imidazole polyamide metallocomplexes

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preparation example Construction

[0301] Compound preparation

[0302] The compounds of the present invention are suitable for preparation in a modular or stepwise manner. Gradual synthesis allows people to change the number and composition of the component polyamides, linkers and metal composites in a controlled manner. For example, the length and composition of the polyamide chain can be selected to target a specific nucleotide sequence. The modular compounds of structural formulas (1), (3), (4) and (5) can be connected with other modular compounds, or connected to another metal compound, to generate structural formulas (1), (3) or (5) Compounds with the required number of pyrrole-imidazole polyamides capable of selectively targeting specific polynucleotide sequences. The compounds of the present invention can be prepared, for example, the compounds of structural formula (1), (3), (4) and (5), which can be targeted to contain about 2, 3, 4, 5, 6, 7, 8, 9 or about The polynucleotide sequence of the selected core ...

Embodiment 1

[0355] Synthesis of Im / Py / Py

[0356] The polyamide Im / Py / Py was synthesized by a method similar to Lown et al. (J. Org. Chem., 1985, 50(20), 374-379). The synthesis diagram of Im / Py / Py is shown in figure 1 .

[0357] Methyl-4-nitropyrrole-2-carboxylic acid (1)

[0358] Heat acetic anhydride (8ml) and nitric acid (70%, 1.6mL) to 50°C, heat for 15 minutes, and cool to room temperature. Then the solution was slowly added to the Ac of 1-methyl-2-pyrrole carboxylic acid (2.0g, 0.02mol) cooled to -25°C 2 O (12ml) suspension. The mixture was stirred at -15°C for 30 minutes, warmed to room temperature, and stirring continued for 20 minutes. The mixture was cooled to -25°C again, and the resulting precipitate was collected in a funnel cooled with dry ice. Use cold Ac 2 O(-25℃) wash, then Ac 2 O: CCl 4 (1:1, -25℃) wash, then use CCl 4 Wash with hexane. The yellow solid was dissolved in NaOH (1M) and acidified with HCl to produce a microemulsion solid product, which was col...

Embodiment 2

[0378] DNA melting experiment

[0379] A Cary 1E recording spectrometer equipped with a Peltier controllable sample cell holder and a sample cell with a length of 1 cm was used to obtain the DNA melting curve graph of Im / Py / Py-Pt at 260 nm. The heating rate in all experiments is 0.5°C / min. The solution conditions were sodium phosphate (10mM), EDTA (1mM) and NaCl (40mM), and the pH was adjusted to 7.0. DNA melting curve such as figure 2 Shown.

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Abstract

The present invention relates to sequence selective compounds for targeting therapeutic or diagnostic groups to polynucleotides. More particularly, the present invention relates to sequence selective targeting of metallocomplexes, such as metallodrugs and metallodiagnostics, to polynucleotides.

Description

Technical field [0001] The present invention relates to sequence-selective compounds that target therapeutic or diagnostic groups to polynucleotides. More specifically, the present invention relates to the selective targeting of polynucleotides such as metal complex sequences of metal drugs and metal diagnostic agents. Background technique [0002] Cisplatin is a metal anticancer drug that binds irreversibly to the nitrogen (N7) of guanine (G) and adenine (A) and forms intra-chain and inter-chain cross-links in the major grooves of DNA. And stop the replication in the cell. However, cisplatin binds indiscriminately, and it also binds to large molecules other than DNA. This indiscriminate combination may cause side effects on healthy cells. Currently, cisplatin is used to treat a variety of cancers, including testicular cancer, ovarian cancer, bladder cancer, head and neck cancer, lung cancer, and cervical cancer. However, the disadvantage of cisplatin is that many human cancer ce...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D207/34A61K31/40A61K31/4164A61P31/12A61P31/18A61P35/00C07D209/56C07D233/90C07D403/14C07D471/04C07D471/14
CPCA61K31/40A61K31/4164A61P31/12A61P31/18A61P35/00C07D403/14C07D471/04C07D471/14Y10T436/143333
Inventor D·哈拉米略C·布罗迪W·霍华德R·塔利布J·奥尔德里奇-赖特
Owner UNIVERSITY OF WESTERN SYDNEY
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