Title:
ANTI-TUMOR COMPOUNDS, AND PREPARATION AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2021/190142
Kind Code:
A1
Abstract:
The present invention relates to anti-tumor compounds, and preparation and uses thereof, which are compounds that can inhibit CK2 protein kinases and cancer cell dryness. Novel compounds as shown in formula II are provided by introducing, by means of an amide bond, an ester bond, and a thioester bond, a fatty chain or heterocyclic structure fragment containing an amino group, a hydroxyl group, a mercapto group, or halogen atoms in a known CK2 inhibitor (CX-4945) parent structure; the compounds have significant anti-cancer activity, and some of the compounds have better cytotoxic activity against cancer cells, better inhibition ability to CK2 protein kinases, and better selectivity to CK2 proteins than parent compounds thereof; in addition, some compounds exhibit a strong inhibition ability to cancer cell dryness, and facilitate overcoming drug resistance; the compounds having structures as shown in formula II-A, formula II-B, formula II-C, formula II-D, and formula II-E are as follows; the compounds of the present invention have a good inhibitory effect on proliferation of cancer cells, can also inhibit cancer cell dryness, and can be used for preparing anti-tumor drugs.
Inventors:
GOU SHAOHUA (CN)
WANG YUANJIANG (CN)
WANG YUANJIANG (CN)
Application Number:
PCT/CN2021/074623
Publication Date:
September 30, 2021
Filing Date:
February 01, 2021
Export Citation:
Assignee:
UNIV SOUTHEAST (CN)
International Classes:
A61P35/00; C07D471/04
Domestic Patent References:
| WO2012054493A1 | 2012-04-26 |
Foreign References:
| CN102036561A | 2011-04-27 | |||
| CN101528704A | 2009-09-09 | |||
| CN102481289A | 2012-05-30 |
Other References:
FABRICE PIERRE; ERIC STEFAN; ANNE-SOPHIE NDELLEC; MARIE-CLAIRE CHEVREL; COLLIN F. REGAN; ADAM SIDDIQUI-JAIN; DIWATA MACALINO; NICO: "7-(4-1,2,4-Triazol-3-yl)benzo[][2,6]naphthyridines: A novel class of Pim kinase inhibitors with potent cell antiproliferative activity", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, ELSEVIER, AMSTERDAM, NL, vol. 21, no. 22, 15 September 2011 (2011-09-15), AMSTERDAM, NL, pages 6687 - 6692, XP028320719, ISSN: 0960-894X, DOI: 10.1016/j.bmcl.2011.09.059
CHEN HONG, FEIHONG CHEN, NANNAN LIU, XINYI WANG, SHAOHUA GOU: "Chemically induced degradation of CK2 by proteolysis targeting chimeras based on a ubiquitin–proteasome pathway", BIOORGANIC CHEMISTRY, vol. 81, 12 September 2018 (2018-09-12), pages 536 - 544, XP055853274, DOI: 10.1016/j.bioorg.2018.09.005
PIERRE F, CHUA P C, O'BRIEN S E, SIDDIQUI-JAIN A, BOURBON P, HADDACH M, MICHAUX J, NAGASAWA J, SCHWAEBE M K, STEFAN E, VIALETTES A: "Discovery and SAR of 5-(3-Chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic Acid (CX-4945), the First Clinical Stage Inhibitor of Protein Kinase CK2 for the treatment of Cancer", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, US, vol. 54, no. 2, 27 January 2011 (2011-01-27), US, pages 635 - 654, XP002715731, ISSN: 0022-2623, DOI: 10.1021/jm101251q
CHEN HONG, FEIHONG CHEN, NANNAN LIU, XINYI WANG, SHAOHUA GOU: "Chemically induced degradation of CK2 by proteolysis targeting chimeras based on a ubiquitin–proteasome pathway", BIOORGANIC CHEMISTRY, vol. 81, 12 September 2018 (2018-09-12), pages 536 - 544, XP055853274, DOI: 10.1016/j.bioorg.2018.09.005
PIERRE F, CHUA P C, O'BRIEN S E, SIDDIQUI-JAIN A, BOURBON P, HADDACH M, MICHAUX J, NAGASAWA J, SCHWAEBE M K, STEFAN E, VIALETTES A: "Discovery and SAR of 5-(3-Chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic Acid (CX-4945), the First Clinical Stage Inhibitor of Protein Kinase CK2 for the treatment of Cancer", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, US, vol. 54, no. 2, 27 January 2011 (2011-01-27), US, pages 635 - 654, XP002715731, ISSN: 0022-2623, DOI: 10.1021/jm101251q
Attorney, Agent or Firm:
NANJING SUGAO PATENT AND TRADEMARK FIRM ( ORDINARY PARTNERSHIP ) (CN)
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