With substituted pyrazine and imidazole derivatives, their preparation and their use in medicine (by machine translation)
The invention discloses a substituted pyrazine and imidazole derivatives, their preparation and their use in medicine. Specifically, the invention relates to a compound of general formula (I) indicated by the new derivative and its pharmaceutically acceptable salt or pharmaceutical composition containing the same, and its preparation method. The invention also discloses the derivative and its pharmaceutically acceptable salt or pharmaceutical composition containing the same in the Bruton tyrosine kinase inhibitors, and in preparing and treating and/or preventing tumor diseases such as inflammation of the application of the medicament. Wherein the general formula (I) of each substituent as defined in the specification. (by machine translation)
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Paragraph 0157; 0159; 0160; 0161; 0162
(2017/10/12)
SUBSTITUTED 4-ARYLOXY AND 4-ARYLSULFANYL-PHENYL-2-AMINOTHIAZOLES AS INHIBITORS OF CELL PROLIFERATION
The invention discloses compounds which are substituted 4-aryloxy and 4-arylsulfanyl-phenyl-2-aminothiazoles with anti-cancer activity. The invention futher discloses methods of preparing compounds of the invention. The invention also discloses methods of inhibiting cell proliferation and tumor growth in a subject by administering compounds of the invention to the subject.
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Page/Page column 30-33
(2008/06/13)
Synthesis and evaluation of substituted 4-aryloxy- and 4-arylsulfanyl- phenyl-2-aminothiazoles as inhibitors of human breast cancer cell proliferation
Several substituted 4-aryloxy- and 4-arylsulfanyl-phenyl-2-aminothiazoles were synthesized and evaluated for cytotoxic activity against estrogen-positive, estrogen-negative, and adriamycin-resistant human breast cancer cell lines. 4-[4′-(3,4-Dichlorophenoxy)-phenyl]-thiazol-2-yl ammonium iodide demonstrated potent activity against both estrogen-positive and negative breast cancer cell lines with low micromolar (μM) GI50 values. In addition, we have identified several 2-aminothiazoles that demonstrated selective potency for the adriamycin-resistant and estrogen-negative breast cancer cell lines. The results suggest that these 2-aminothiazoles represent lead compounds for evaluation in animal models of breast cancer.
Gorczynski, Michael J.,Leal, Rachel M.,Mooberry, Susan L.,Bushweller, John H.,Brown, Milton L.
p. 1029 - 1036
(2007/10/03)
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