- CALPAIN MODULATORS AND THERAPEUTIC USES THEREOF
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Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof.
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- Synthesis and biological evaluation of aryloxazole derivatives as antimitotic and vascular-disrupting agents for cancer therapy
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A series of aryloxazole, thiazole, and isoxazole derivatives was synthesized as vascular-targeting anticancer agents. Antiproliferative activity and tumor vascular-disrupting activity of all of the synthesized compounds were tested in vitro using various human cancer cell lines and HUVECs (human umbilical vein endothelial cells). Several compounds with an arylpiperazinyl oxazole core showed excellent cytotoxicity and metabolic stability in vitro. Among this series, two representative compounds (6-48 and 6-51) were selected and tested for the evaluation of anticancer effects in vivo using tumor-bearing mice. Compound 6-48 effectively reduced tumor growth (42.3% reduction in size) at the dose of 100 mg/kg. We believe that compound 6-48 will serve as a good lead compound for antimitotic and vascular-disrupting agents; further investigation to improve the in vivo efficacy of this series is underway.
- Choi, Min Jeong,No, Eun Sun,Thorat, Dhanaji Achyutrao,Jang, Jae Wan,Yang, Hakkyun,Lee, Jaeick,Choo, Hyunah,Kim, Soo Jin,Lee, Chang Sik,Ko, Soo Young,Lee, Jiyoun,Nam, Ghilsoo,Pae, Ae Nim
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p. 9008 - 9018
(2014/01/06)
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- A general and efficient PIFA mediated synthesis of heterocycle-fused quinolinone derivatives
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A new application of the hypervalent iodine reagent phenyliodine(III)bis(trifluoroacetate) (PIFA) has been developed for the construction of a series of N, O, S-containing heterocycle-fused quinolinone derivatives in a general and efficient way. An altern
- Herrero, M.Teresa,Tellitu, Imanol,Domínguez, Esther,Hernández, Susana,Moreno, Isabel,SanMartín, Raúl
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p. 8581 - 8589
(2007/10/03)
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- Azole-phenyl urea derivatives as ACAT inhibitors and their production
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The present invention relates to azole-phenyl urea derivatives represented by the general formula (I): [wherein each of R1, R2and R3is H, halogen, C1-8alkyl or the like, and A is a group represented by the formula (i) or (ii): (wherein R4, R5, R6and X are as defined in the specification.)] and a pharmacologically acceptable salt thereof, which have ACAT-inhibitory activity and are useful as a prophylactic and therapeutic agent for hypercholesterolemia, atherosclerosis and various diseases caused by them; a process for producing said derivative; and an ACAT inhibitor containing said derivative or salt as an active ingredient.
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