- Synthesis of aminoquinazoline derivatives and their antiproliferative activities against melanoma cell line
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The synthesis of a novel series of aminoquinazoline derivatives 1a-r and their antiproliferative activities against A375 human melanoma cell line were described. Among them, six compounds showed superior antiproliferative activities to Sorafenib as a reference compound. In particular, the representative compound 1q bearing chromen-4-one moiety exhibited excellent antiproliferative activity (IC50 = 0.006 μM) and good selectivity over HS27 fibroblast cell line.
- Lee, Junsang,Nam, Bong Soo,Kim, Hwan,Oh, Chang-Hyun,Lee, So Ha,Cho, Seung Joo,Sim, Tae Bo,Hah, Jung-Mi,Kim, Dong Jin,Tae, Jinsung,Yoo, Kyung Ho
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scheme or table
p. 5722 - 5725
(2010/11/24)
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- CRYSTAL FORM OF PHENYLAMINO PYRIMIDINE DERIVATIVES
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The present invention relates to a particular form of the (3,5-bis trifluoromethyl)-N-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide (formula I), processes for the preparation thereof, pharmaceutical compositions containing this crystal form, and their use as anti tumor agent in humans. The compound of formula I, also known as AN-019, is:
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Page/Page column 10
(2009/09/25)
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- NOVEL PHENYLAMINOPYRIMIDINE DERIVATIVES AS INHIBITORS OF BCR-ABL KINASE
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The present invention relates to novel intermediates useful for the preparation of novel phenylaminopyrimidine derivatives, novel phenylaminopyrimidine derivatives. Pharmaceutical composition containing the novel phenylaminopyrimidine derivatives and processes for their preparation. The invention particularly relates to novel Phenyl pyrimidine amine derivatives of the general formula (I). The novel compounds of the formula 1 can be used in the therapy of Chronic Myeloid Leukemia (CML). Since the IC50; 191 values of these molecules are in the range 0.1 to 10.0 nm, these novel compounds are potentially useful for the treatment of CML.
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Page/Page column 28-29
(2008/06/13)
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