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Cancer treatments targeting cancer stem cells

A single ring, compound technology, applied in the direction of tumor/cancer cells, animal cells, vertebrate cells, etc., can solve the problem of drug-resistant tumor cancer spread and other problems

Pending Publication Date: 2021-02-02
治疗方案股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

3，4 Because current treatments do not target cancer stem cell populations, they often lead to the emergence of drug-resistant tumors and continued cancer spread

Method used

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  • Cancer treatments targeting cancer stem cells
  • Cancer treatments targeting cancer stem cells
  • Cancer treatments targeting cancer stem cells

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0782] Example 1. Kinetic cell viability of AGS cells

[0783]Approximately 50,000 AGS cells were seeded into each well of a 96-well plate in medium containing NanoLuc luciferase and the MT cell viability substrate provided in PROMEGA's RealTime Glo MT Cell Viability Assay Kit. Four hours after plating, cells were treated with DMSO alone (no drug treatment) or decreasing concentrations of compounds of the disclosure to achieve final concentrations of 20, 10, 5, and 2.5 μΜ. Luminescent units (RLU) were measured every 16-20 hours using a SynergyHTX plate reader with 30 msec integration (see figure 1 ).

Embodiment 2

[0784] Example 2. Human Microarray Studies

[0785] AGS human gastric adenocarcinoma cells were treated with compound 1-1 or DMSO alone (as a negative control) for two days. Two days later, RNA was isolated in duplicate from Compound 1-1-treated cells and DMSO-treated cells, and microarray analysis was performed using the AFFYMETRIX CLARIOM S microarray. Data are expressed as fold change relative to Compound I-1-treated cells, with negative values ​​denoting genes that are higher in Compound I-1-treated cells than in DMSO-treated cells, while positive values ​​denote genes that are higher in DMSO-treated cells Than higher genes in compound 1-1 treated cells. Values ​​from replicate samples were averaged. Data were included for genes whose expression was changed more than 3-fold up or down in response to compound 1-1.

[0786] Table 1 shows the list of genes up-regulated after treatment of AGS human gastric cancer cell line with compound I-1 (shown below). Negative numbers ...

Embodiment 3

[0798] Example 3. Kinetic Cell Viability of AGS Cells

[0799] Compound 1-1 was tested for its ability to inhibit the growth of 12 additional cell lines derived from a variety of different types of human cancers. In addition to the effective inhibition of gastric adenocarcinoma and gastrointestinal stromal cell growth (gastric adenocarcinoma data shown in Example 1, gastrointestinal stromal tumor data shown in Table 3), compound I-1 also inhibited the growth of non-cholesterol Chickkin's lymphoma, small cell lung cancer, pancreatic cancer, gastrointestinal stromal and ovarian adenocarcinoma cells had the most potent effects. Exemplary results are shown in Table 3. IC 50 Values ​​are listed, and the IC50 value is the lowest concentration of Compound 1-1 that results in 50% inhibition of cancer cell growth.

[0800] table 3.

[0801] cell line cancer type IC 50 (μM)

IGROV-1 ovarian adenocarcinoma 4.54 NCI-H69 Small Cell Lung Cancer 1.50 ...

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PUM

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Abstract

Disclosed are compounds, methods, compositions, and kits that allow for treating cancer by, e.g., targeting cancer stem cells. In some embodiments, the cancer is colorectal cancer, gastric cancer, gastrointestinal stromal tumor, ovarian cancer, lung cancer, breast cancer, pancreatic cancer, prostate cancer, testicular cancer, or lymphoma. In some embodiments, the cancer is liver cancer, endometrial cancer, leukemia, or multiple myeloma. The compounds utilized in the disclosure are of Formula (0), (O'), and (I):.

Description

[0001] related application [0002] This application claims priority under Title 35, United States Code, Section 119(e) of U.S. Provisional Applications U.S.S.N. 62 / 667,412, filed May 4, 2018, and U.S.S.N. The contents are each incorporated herein by reference. Background technique [0003] Cancer is ubiquitous and, despite advances in medicine, remains the leading cause of death worldwide. In 2017, an estimated 1.7 million new cases of cancer were diagnosed and 600,000 people died from the disease. 1 Cancer is the second leading cause of death worldwide, with nearly one in six deaths due to cancer. Over the next 20 years, the number of new cases is expected to increase by approximately 70%. The economic impact of cancer is enormous and increasing. The total annual economic cost of cancer was estimated to be about $1.16 trillion in 2010. 2 [0004] Cancer is a general term for a large group of diseases that can affect any part of the body. Other terms used are malignanc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/165A61K31/505A61K31/506C07D239/00C07D239/02C07D239/24
CPCA61K31/506C07D401/12C07D401/14C07D403/12C07D209/08A61P35/00C07D405/12C07D413/12C07D213/73A61K45/06A61K31/4439A61K31/444A61K31/404A61K31/4178A61K31/501A61K31/422A61K31/4155A61K31/454A61K31/4406A61K31/4709A61K31/52A61K31/519C12N5/0695A61K2300/00C07D213/81C07D487/04C07D473/00C07D209/04C07D413/14C07D213/56
Inventor G.T.克里明斯D.A.德杰瑟斯迪亚兹Y.布鲁思-阿尔-科尔
Owner 治疗方案股份有限公司
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