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  1. Article: The synthesis of anticancer sulfonated indolo[2,1-a]isoquinoline and benzimidazo[2,1-a]isoquinolin-6(5H)-ones derivatives via a free radical cascade pathway

    Pan, You-lu / Gong, Xiao-meng / Hao, Rong-rong / Zeng, Shen-xin / Shen, Zheng-rong / Huang, Wen-hai

    RSC advances. 2022 Mar. 29, v. 12, no. 16

    2022  

    Abstract: A facile CuBr₂ induced radical relay addition/cyclization of activated alkenes with substituted-thiosulfonates has been achieved, leading to a broad range of sulfonated indolo[2,1-a]isoquinolines and benzimidazo[2,1-a]isoquinolin-6(5H)-ones in moderate ... ...

    Abstract A facile CuBr₂ induced radical relay addition/cyclization of activated alkenes with substituted-thiosulfonates has been achieved, leading to a broad range of sulfonated indolo[2,1-a]isoquinolines and benzimidazo[2,1-a]isoquinolin-6(5H)-ones in moderate to good yields. In particular, some compounds exhibit bioactivity against cancer cell lines. This protocol shows advantages of low-cost, base-free, simple operation, and broad functional group tolerance.
    Keywords alkenes ; bioactive properties ; free radicals ; isoquinolines ; neoplasm cells
    Language English
    Dates of publication 2022-0329
    Size p. 9763-9772.
    Publishing place The Royal Society of Chemistry
    Document type Article
    ISSN 2046-2069
    DOI 10.1039/d1ra06981k
    Database NAL-Catalogue (AGRICOLA)

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  2. Article ; Online: The synthesis of anticancer sulfonated indolo[2,1-

    Pan, You-Lu / Gong, Xiao-Meng / Hao, Rong-Rong / Zeng, Shen-Xin / Shen, Zheng-Rong / Huang, Wen-Hai

    RSC advances

    2022  Volume 12, Issue 16, Page(s) 9763–9772

    Abstract: ... A facile ... ...

    Abstract A facile CuBr
    Language English
    Publishing date 2022-03-29
    Publishing country England
    Document type Journal Article
    ISSN 2046-2069
    ISSN (online) 2046-2069
    DOI 10.1039/d1ra06981k
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: The copper-catalyzed oxidation of arylmethyl triazines with H

    Zeng, Ming / Yuan, Zi-Xin / Wen, Lin-Fei / Jiang, Dengzhao / Lu, Hui / Liu, Wenbo / Dai, Jun / Zeng, Shen-Xin

    Organic & biomolecular chemistry

    2022  Volume 20, Issue 27, Page(s) 5406–5411

    Abstract: We report an efficient copper-catalyzed dehydrogenation method for the synthesis of aroyl triazines from arylmethyl triazines with water in the absence of additional oxidants or hydrogen acceptors. The use of substrates with both electron-donating and ... ...

    Abstract We report an efficient copper-catalyzed dehydrogenation method for the synthesis of aroyl triazines from arylmethyl triazines with water in the absence of additional oxidants or hydrogen acceptors. The use of substrates with both electron-donating and electron-withdrawing groups resulted in moderate to good yields. Using liquid chromatography-mass spectrometry,
    MeSH term(s) Catalysis ; Copper/chemistry ; Hydrogen ; Oxidants/chemistry ; Triazines/chemistry ; Water
    Chemical Substances Oxidants ; Triazines ; Water (059QF0KO0R) ; Copper (789U1901C5) ; Hydrogen (7YNJ3PO35Z)
    Language English
    Publishing date 2022-07-13
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2097583-1
    ISSN 1477-0539 ; 1477-0520
    ISSN (online) 1477-0539
    ISSN 1477-0520
    DOI 10.1039/d2ob00582d
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: The progress of small-molecules and degraders against BCR-ABL for the treatment of CML.

    Pan, You-Lu / Zeng, Shen-Xin / Hao, Rong-Rong / Liang, Mei-Hao / Shen, Zheng-Rong / Huang, Wen-Hai

    European journal of medicinal chemistry

    2022  Volume 238, Page(s) 114442

    Abstract: Chronic myeloid leukemia (CML) is a malignant disease of the hematopoietic system with crucial pathogenic protein named BCR-ABL, which endangers the life of patients severely. As a milestone of targeted drug, Imatinib has achieved great success in the ... ...

    Abstract Chronic myeloid leukemia (CML) is a malignant disease of the hematopoietic system with crucial pathogenic protein named BCR-ABL, which endangers the life of patients severely. As a milestone of targeted drug, Imatinib has achieved great success in the treatment of CML. Nevertheless, inevitable drug resistance of Imatinib has occurred frequently in clinical due to the several mutations in the BCR-ABL kinase. Subsequently, the second-generation of tyrosine kinase inhibitors (TKIs) against BCR-ABL was developed to address the mutants of Imatinib resistance, except T315I. To date, the third-generation of TKIs targeting T315I has been developed for improving the selectivity and safety. Notably, the first allosteric inhibitor has been in market which could overcome the mutations in ATP binding site effectively. Meanwhile, some advanced technology, such as proteolysis-targeting chimeras (PROTAC) based on different E3 ligand, are highly expected to overcome the drug resistance by selectively degrading the targeted proteins. In this review, we summarized the current research progress of inhibitors and degraders targeting BCR-ABL for the treatment of CML.
    MeSH term(s) Antineoplastic Agents/pharmacology ; Antineoplastic Agents/therapeutic use ; Benzamides/therapeutic use ; Drug Resistance, Neoplasm ; Fusion Proteins, bcr-abl ; Humans ; Imatinib Mesylate/therapeutic use ; Leukemia, Myelogenous, Chronic, BCR-ABL Positive/drug therapy ; Leukemia, Myelogenous, Chronic, BCR-ABL Positive/pathology ; Piperazines/pharmacology ; Protein Kinase Inhibitors/pharmacology ; Protein Kinase Inhibitors/therapeutic use ; Pyrimidines/pharmacology
    Chemical Substances Antineoplastic Agents ; Benzamides ; Piperazines ; Protein Kinase Inhibitors ; Pyrimidines ; Imatinib Mesylate (8A1O1M485B) ; Fusion Proteins, bcr-abl (EC 2.7.10.2)
    Language English
    Publishing date 2022-05-06
    Publishing country France
    Document type Journal Article ; Review
    ZDB-ID 188597-2
    ISSN 1768-3254 ; 0009-4374 ; 0223-5234
    ISSN (online) 1768-3254
    ISSN 0009-4374 ; 0223-5234
    DOI 10.1016/j.ejmech.2022.114442
    Database MEDical Literature Analysis and Retrieval System OnLINE

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