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Synthetic rigidin analogues as Anti-cancer agents, salts, solvates and prodrugs thereof, and method of producing same

A compound and fusion technology, applied in antineoplastic drugs, pharmaceutical formulations, drug combinations, etc., can solve problems such as no chemical synthesis, no biological properties, weak anti-proliferation and calmodulin antagonistic activity

Inactive Publication Date: 2018-01-02
NEW MEXICO TECH RES FOUND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although these natural products have been reported to have weak anti-proliferative and calmodulin-antagonistic activities, their biological properties have been little studied due to insufficient quantities of the substances available from isolation and no efficient chemical synthesis

Method used

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  • Synthetic rigidin analogues as Anti-cancer agents, salts, solvates and prodrugs thereof, and method of producing same
  • Synthetic rigidin analogues as Anti-cancer agents, salts, solvates and prodrugs thereof, and method of producing same
  • Synthetic rigidin analogues as Anti-cancer agents, salts, solvates and prodrugs thereof, and method of producing same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Example 1. 6-benzoyl-5-(3,5-dibromophenyl)-1H-pyrrolo[2,3-d]pyrimidin-4(7H)-one (Rig8): 77%;

[0049]

[0050] HRMS m / z (ESI) C 19 h 12 Br 2 N 3 o 2 (M+H + ) calculated value: 471.9296, measured value: 471.9301.

Embodiment 2

[0051] Example 2. 6-benzoyl-5-(5-bromopyridin-3-yl)-1H-pyrrolo[2,3-d]pyrimidin-4(7H)-one (Rig9): 88%;

[0052]

[0053] HRMS m / z (ESI) C 18 h 11 BrN 4 NaO 2 (M+Na + ) calculated value: 416.9963, measured value: 416.9965.

Embodiment 3

[0054] Example 3. 5-(3,5-dibromophenyl)-6-(4-methoxybenzoyl)-1H-pyrrolo[2,3-d]pyrimidin-4(7H)-one ( Rig10): 60%;

[0055]

[0056] HRMS m / z (ESI) C 20 h 13 Br 2 N 3 NaO 3 (M+Na + ) calculated value: 523.9221, measured value: 523.9221.

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PUM

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Abstract

A compound having the Formula as follows: (F) wherein R, R1 and R2 are selected from hydrogen, aryl, fused aryl, heteroaryl, saturated carbocylclic, partially saturated carbocyclic, saturated heterocyclic, partially saturated heterocyclic, C1-10 alkyl, haloalkyl, alkenyl, alkynyl, arylalkyl, arylalkenyl, arylalkynyl, heteroarylalkyl, heteroarylalkenyl, alkenylalkyl, alkynylalkyl, carbocycloalkyl,heterocycloalkyl, hydroxyalkyl, aminoalkyl, carboxyalkyl, nitroalkyl, cyanoalkyl, acetamidoalkyl, and acyloxyalkyl. A process for the preparation thereof is also provided.

Description

[0001] This application is a continuation-in-part of US Patent Application Serial No. 13 / 678,987, filed November 16, 2012. Background of the invention [0002] The present invention relates to synthetic rigidin analogs as anticancer agents, to their salts, solvates and prodrugs, and to methods for their production. [0003] Cancer is the second leading cause of death in the United States. Cancer is a group of more than 100 diseases characterized by dysregulated, abnormal cell growth and proliferation. Anticancer agents are one of many different tools used to fight cancer. They can be used alone or in combination with other treatment options to fight the disease. As life expectancy continues to increase and cancer rates are expected to only increase in the future, the development of new anticancer agents is a top priority for the drug development community. Of particular importance are the large number of new anticancer agents derived from natural sources. Only about 20% of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/535
CPCC07D487/04A61P1/00A61P11/00A61P15/08A61P17/00A61P25/28A61P35/00A61P35/04A61K31/519
Inventor 伊戈尔·马格多夫斯内斯娜·罗赫伊莉莉亚·V·弗罗洛娃亚历山大·V·科尼恩科
Owner NEW MEXICO TECH RES FOUND