Semisynthetic aurones and methods of use thereof

A semi-synthetic, auran technology, applied in the application field of semi-synthetic aurone with anti-tumor activity, auran inhibits the growth of cancer cells in patients in need

Pending Publication Date: 2020-10-20
UNIV OF KENTUCKY RES FOUND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, due to the reported variety of effects, ca...

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  • Semisynthetic aurones and methods of use thereof
  • Semisynthetic aurones and methods of use thereof
  • Semisynthetic aurones and methods of use thereof

Examples

Experimental program
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Embodiment

[0090] Prior to this example, certain aurones were known, but were not considered practical antineoplastic agents due to their limited potency and uncertain biological, cellular targets. In particular, published work has led to semi-synthetic aurones with varying levels of antitumor activity: with 2-(coumarin-4-yl)methylene and 2-(furan-2-yl)methylene Benzofuran-3(2 / / )-one is active against human leukemia K562 cells; benzofuran-3(2 / / )-one with 2-(piperazin-l-yl)methylene is active against A solid tumor cell line has IC50 values ​​in the low micromolar range; The cell proliferation of -231 cell line has inhibitory effect. However, the relative potency among these heteroaryl-substituted aurones, and in these cases the specific biological target(s) remains unknown.

[0091] With this in mind, structure-activity (SAR) studies involving modifications of the C-6 hydroxyl and C-2 benzylidene subunits found in many naturally occurring aurones were performed. See Scenario 1 below. ...

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PUM

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Abstract

Provided herein are semisynthetic aurones, pharmaceutical compositions, and methods of treating cancer. The semisynthetic aurone compound including a structure according to Formula (I) or pharmaceutically acceptable salt thereof, where R1 is H, an alkyl cyano, an alkyl phenyl substituted with one or more halogens, or any combination thereof, and R2 is an aromatic group, a heterocycle, or a combination thereof. The pharmaceutical composition includes the semisynthetic aurone compound and a carrier. The method includes administering to a patient in need of such treatment an effective amount of the semisynthetic aurone compound.

Description

[0001] related application [0002] This application claims the benefit of U.S. Provisional Application Serial No. 62 / 620,120, filed January 22, 2018, which is hereby incorporated by reference in its entirety. [0003] government interest [0004] In Contract Nos. R00 CA181500; R01 CA172379; DP2 CA228043 and R21 CA205108 awarded by the National Institutes of Health, and P20 RR020171 and P30GM110787 awarded by the National Institute of General Medical Sciences The invention is carried out under the support of No. contract. The government has certain rights in this invention. technical field [0005] The present disclosure relates to semi-synthetic aurones and methods of their use. In particular, the disclosure relates to semi-synthetic aurones having antitumor activity, and the use of such aurones to inhibit the growth of cancer cells, such as leukemia, colon, prostate, breast or lung cancer, in a patient in need thereof. Background technique [0006] Aurone contains rela...

Claims

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Application Information

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IPC IPC(8): A61K31/343C07D307/83C07D405/06
CPCC07D307/83C07D405/06A61P35/00C07D405/10C07D413/10C07D417/10
Inventor J·S·布莱克本M·弗朗斯纽克刘春明谢彦奇D·S·瓦特
Owner UNIV OF KENTUCKY RES FOUND
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