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Hydrocarbyl tin complex with antitumor activity and preparation method thereof

A technology of anti-tumor activity and complexes, which is applied in the direction of anti-tumor drugs, compounds of group 4/14 elements of the periodic table, compounds of group 5/15 elements of the periodic table, etc. There are few researches on the anti-tumor activity of drugs, etc.

Inactive Publication Date: 2020-06-26
台州泰捷化工科技有限公司
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  • Summary
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  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There have been literature reports on the research on the hydrocarbyl tin complexes of alkynylphosphonic acid, but these literatures mostly focus on the synthesis and structure research stage, and there are few studies on pharmacological activity, and most of them are tested for their bactericidal and acaricidal activities. , there are few studies on the antitumor activity of such complexes

Method used

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  • Hydrocarbyl tin complex with antitumor activity and preparation method thereof
  • Hydrocarbyl tin complex with antitumor activity and preparation method thereof
  • Hydrocarbyl tin complex with antitumor activity and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1 3

[0016] Synthesis of embodiment 1 tri-n-butyltin (IV) (4-methoxyphenyl) ethynyl phosphonic acid derivative

[0017]

[0018] The structural formula of the product is:

[0019] In a 100mL round bottom flask, add 3mmol tri-n-butyltin chloride and 20mL anhydrous methanol, stir, after tributyltin chloride is completely dissolved, add 3.2mmol (4-methoxyphenyl) ethynyl phosphoric acid Monosodium, stirred and reacted under reflux for 4.5 hours, cooled, filtered, the filtrate was concentrated under reduced pressure, an appropriate amount of petroleum ether was added and filtered, and concentrated in vacuo to obtain the product with a yield of 87%.

[0020] Elemental analysis data: Anal.Calcd.For C 21 h 35 o 4 PSn (%): C 53.33, H 7.04, Sn 23.69; Found (%): C 53.37, H 7.06, Sn 23.73. H NMR spectrum data: 1 H NMR / δ 0.79-0.83(9H), 1.24-2.03(18H), 3.42-4.02(3H), 7.33-7.90(4H).

Embodiment 2

[0022] According to the method of Example 1, monosodium phenylethynyl phosphate was selected as a raw material to prepare tri-n-butyltin (IV) phenylethynylphosphonic acid derivatives.

Embodiment 3

[0023] The antitumor activity test of embodiment 3 compound

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Abstract

The invention provides a hydrocarbyl tin complex with antitumor activity and a preparation method thereof. And the activity of the hydrocarbyl tin complex is tested, and the hydrocarbyl tin complex shows much stronger activity than cis-platinum, especially has very high activity on human colon cancer, and is a potential candidate of clinical antitumor drugs.

Description

technical field [0001] The invention relates to a hydrocarbyl tin complex of alkynyl phosphonic acid with antitumor activity, belonging to the field of medicinal chemistry. Background technique [0002] Phosphine (phosphoric) acid derivatives of hydrocarbyl tin have strong biological activities such as insecticidal, bactericidal and herbicidal, and have received great attention from people. There have been literature reports on the research on the hydrocarbyl tin complexes of alkynylphosphonic acid, but these literatures mostly focus on the synthesis and structure research stage, and there are few studies on pharmacological activity, and most of them are tested for their bactericidal and acaricidal activities. , There are few studies on the antitumor activity of this kind of complexes. [0003] Tin complexes usually have certain anti-tumor activity. Based on this consideration, in order to explore new anti-cancer drugs, we carried out an investigation on the existing litera...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/40A61P35/00
CPCA61P35/00C07F9/4056C07F9/4071C07F9/4015C07F7/226
Inventor 金建德
Owner 台州泰捷化工科技有限公司
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