2976-31-0Relevant academic research and scientific papers
Aniline pyrimidines, its preparation method and medical use (by machine translation)
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Paragraph 0126; 0127; 0128, (2018/03/01)
The invention relates to: an aniline pyrimidine compound represented as the formula (I), a medicinal salt thereof, a prodrug thereof, and a hydrate or solvate thereof and also relates to: the preparation method of the compound, a medicine composition comp
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.
PYRROLE DERIVATIVES AND THEIR METHODS OF USE
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Page/Page column 63, (2008/06/13)
The invention relates to a series of substituted pyrrole derivatives, compositions comprising the same, and methods of treating conditions and disorders using such compounds and compositions.
Pteridinone derivatives as PI3-kinases inhibitors
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Page/Page column 16, (2008/12/07)
New compounds of formula 1 are provided which by virtue of their pharmaceutical activity as PI3-kinase modulators may be used in the therapeutic field for the treatment of inflammatory or allergic diseases. Examples of these include inflammatory and allergic respiratory complaints, inflammatory diseases of the gastro-intestinal tract and motor apparatus, inflammatory and allergic skin diseases, inflammatory eye diseases, diseases of the nasal mucosa, inflammatory or allergic conditions involving autoimmune reactions or inflammations of the kidney.
Syntheses of Some Alkyl, Cycloalkyl and Aryl 3-Aminophenyl Sulfones
Courtin, Alfred
, p. 1849 - 1853 (2007/10/02)
Syntheses of alkyl (1a-1i, 1m), cycloalkyl (1j, 1k) and aryl (1l) 3-aminophenyl sulfones were achieved by ethanolic Bechamp-reduction of the appropriate 3-nitrophenyl sulfones (3a-3m).The alkyl (3a-3i) and cycloalkyl (3j, 3k) 3-nitrophenyl sulfones were p
