2924-67-6Relevant academic research and scientific papers
Iodine-Mediated Sulfenylation of Imidazo[1,2- a ]pyridines with Ethyl Arylsulfinates
Sun, Jian,Mu, Yangxiu,Iqbal, Zafar,Hou, Jing,Yang, Minghua,Yang, Zhixiang,Tang, Dong
supporting information, p. 1014 - 1018 (2021/03/15)
A simple iodine-mediated approach is reported for the synthesis of sulfenylated imidazo[1,2- a ]pyridines through the reaction of imidazo[1,2- a ]pyridines with ethyl arylsulfinates under mild conditions. The reaction scope was investigated, and a plausible mechanism is proposed to elucidate the reaction process and activation mode. The results indicate that ethyl sulfinates are efficient sulfur sources for the construction of C-S bonds.
PYRAZOLYL COMPOUNDS AND METHODS OF USE THEREOF
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, (2020/05/14)
Compounds having activity as chemotherapeutic agents are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, stereoisomer, isotopic form or prodrug thereof, wherein R1a, R1b, R1c, R1d, L, and are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods for treating cancer (e.g., hematological cancers) are also provided.
Bromine structural domain inhibitor compound and application thereof
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, (2019/08/02)
The invention relates to a bromine structural domain inhibitor and provides a compound shown in a general formula I, pharmaceutical salt, an enantiomer, a diastereoisomer, an atropisomer, racemate, apolymorphic substance and solvate of the compound or an isotope labelled compound (including a deuterium substituted compound), a preparation method of the compound, pharmaceutical composition containing the compound and an application of the above components in pharmaceuticals.
COMPOUNDS AND COMPOSITIONS FOR TREATMENT OF BREAST CANCER
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Paragraph 0109, (2018/10/21)
The present invention provides novel methods of treating triple-negative breast cancer (TNBC). In certain embodiments, the methods of the invention do not require the use of ionizing radiation therapies. In other embodiments, the methods of the invention do not harm non-cancerous cells.
BROMODOMAIN INHIBITORS
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, (2018/04/27)
Provided are compounds of formula (I),wherein R 1, Y, X 1, X 2, R 2, R 3, R 4, R 5, R 6 and m have any of the values defined in the specification and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising compounds of formula (I).
Imidazo pyrazine compound, medicine composition of imidazo pyrazine compound and purpose of imidazo pyrazine compound
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, (2016/10/08)
The invention provides an imidazo pyrazine derivative, a preparation method of the imidazo pyrazine derivative and a purpose of the imidazo pyrazine derivative as medicine. The invention provides a compound shown by a formula (I) and a physiologically acceptable salt, wherein each sign is defined as the specification. The compound can be combined with protein having the bromodomain structure domain so as to regulate the downstream signal path and to achieve a specific function; the compound can be used for various diseases relevant to the bromodomain structure domain protein; the compound can interfere with the combination of the acetylated histone and the Brd4 with the bromodomain structure domain; further, the transcription of the cancer gene and other relevant target genes is reduced, so that the compound can become effective treatment medicine for tumor.
BROMODOMAIN INHIBITORS
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, (2014/06/24)
The present invention provides for compounds of formula (I) wherein A1, A2, A3, A4, X1, X2, Y1, L1, G1, Rx, and Ry have any of the values defined thereof in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
DIHYDRO-PYRROLOPYRIDINONE INHIBITORS
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, (2014/09/29)
The present invention provides for compounds of formula (I) wherein R1, R2, R3, R4, and R5 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
BROMODOMAIN INHIBITORS
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, (2015/01/16)
The present invention provides for compounds of formula (I). wherein Rx, Ry, Rx1, L1, G1, A1, A2, A3, and A4 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).
Syntheses and In Vitro Anticancer Properties of Novel Radiosensitizers
Ates-Alagoz, Zeynep,Coleman, Natalia,Martin, Marlena,Wan, Aaron,Adejare, Adeboye
, p. 853 - 861 (2013/01/15)
Series of 4-(ethylsulfonyl)-1-halogen-2-nitrobenzene (3a-e) and 1-(4-halogen-3-nitrophenyl) propan-1-one (5a-d) analogs designed as novel radiosensitizers using bromonitropropiophenone and bromonitrobenzonitrile as lead compounds were synthesized. The anticancer activities of the compounds were evaluated in vitro using human prostate cancer (DU-145) and breast cancer (MCF-7) cell lines and the MTT assay. From the series, six compounds (3b-e, 5b-c) exhibited potent growth inhibitory effects against both cell lines. The most active, compound 3d, is an iodosulfone and is significantly more potent than the lead compound 5c at 10μm. Compounds were then compared with doxorubicin, a clinically used anticancer compound for breast and prostate cancers. Our most active compound 3d is more effective than doxorubicin at the dose level of 10μm at 3days after radiation, cell viabilities of 18%, 13% compared to 87%, 94% against MCF-7, and 15%, 20% compared to 60%, 75% against DU-145 without and with radiation, respectively. At 10μm, compound 5c had no effects as compared to control, whereas compound 3d reduced DU-145 cell viability to 16% and that of MCF-7 cells to 9% even at 5days after radiation. These results are very encouraging. Future studies include testing the compounds in vivo with and without radiation. Our most active compound 3d is significantly more effective than doxorubicin or lead compound 5c at the dose level of 10μm, without and with radiation; and in MCF-7 and DU-145 cell lines. These results are very encouraging. Future studies include testing the compounds in vivo without and with radiation.
