Identification of a potent and noncytotoxic inhibitor of melanin production
摘要:
On the basis of a hit from random screening, biaryl amide derivatives were prepared in a combinatorial manner via parallel solution-phase synthesis, and their effects on melanocytes were investigated to discover new effective skin depigmenting agents. Among the 120 derivatives prepared, five members exhibited a >30% reduction of melanin production at 30 mu M with a cell viability of >90%. In particular, compound A(3)/B-5 exhibited effective inhibitory activity on melanin synthesis. Although the inhibition percentage of A(3)/B-5 was slightly lower than that of the positive reference compound, phenylthiourea (PTU), A(3)/B-5 demonstrated a much better cell viability than PTU. In vivo evaluation of A(3)/B-5 also showed a significant decrease of melanin pigments. In addition, the in silico classification model was built based on the experimental data of library members. Our results suggest that these biaryl amide derivatives may act as potent skin depigmenting agents. (C) 2010 Elsevier Ltd. All rights reserved.
NOVEL BIARYLAMIDE DERIVATIVE AND COMPOSITIONS CONTAINING THE DERIVATIVE AS AN ACTIVE INGREDIENT
申请人:Shin Dong Heon
公开号:US20120289595A1
公开(公告)日:2012-11-15
The present invention relates to a novel biarylamide derivative and a pharmaceutical composition or a cosmetic composition comprising the same as an active ingredient. More particularly, the present invention relates to a novel biarylamide derivative, a pharmaceutical composition or a cosmetic composition for preventing or treating a pigmentation disorder caused by an abnormal excess of melanin or a disease caused by melanocyte hyperplasia comprising the same as an active ingredient. The biarylamide derivative of the present invention inhibits melanin production and thus inhibits melanocyte hyperplasia. Therefore, a cosmetic composition comprising the biarylamide is excellent in a whitening effect, and a pharmaceutical composition comprising the biarylamide is effective in the prevention or treatment of pigmentation disorders of skin such as lentigo, melasma, freckle, etc. and malignant melanoma.
INK FOR INK JET RECORDING, INK JET RECORDING METHOD, INFRARED READING METHOD, AND PRINTED PRODUCT
申请人:FUJIFILM Corporation
公开号:EP3502198A1
公开(公告)日:2019-06-26
Provided is an ink jet recording ink including: a colorant represented by the following Formula 1, in which an absorption maximum of a dry material of the ink jet recording ink is 700 nm to 1000 nm.
The present invention provides a pharmaceutical composition which is useful as a phosphatidylinositol 3 kinase (PI3K) inhibitor and an antitumor agent, and it provides a novel bicyclic or tricyclic fused heteroaryl derivative or a salt thereof which possesses an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity.