150225-96-0Relevant articles and documents
Ortho-aminobenzoic acid derivative and application thereof
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Paragraph 0048-0051, (2020/07/13)
The invention relates to the technical field of cosmetics and medicines, in particular to an ortho-aminobenzoic acid derivative compound and application thereof. By preparing a series of compounds with an anti-inflammatory function, the obtained anti-inflammatory compound can be used for preparing cosmetic reagents or pharmaceutical reagents, and the cosmetic reagents and the pharmaceutical reagents are not specifically limited. For example, the cosmetic can be a smoothing toner, a nutritional toner, a massage cream, an emollient, a gel, a nutritional cream, a mask, a gel or a shower gel shampoo and other washing type cosmetics, and can also be a cream, ointment, cream, plaster or spray and other similar pharmaceutical preparation products. The compound can be used for a sensitive skin andcan also be added to infant and child cosmetics to reduce irritation.
Inhibition of PCAF histone acetyltransferase, cytotoxicity and cell permeability of 2-acylamino-1-(3-or 4-carboxy-phenyl)benzamides
Park, Woong Jae,Ma, Eunsook
, p. 13116 - 13131 (2013/02/22)
Small molecule HAT inhibitors are useful tools to unravel the role of histone acetyltransferases (HATs) in the cell and they also have relevance in oncology. We synthesized a series of 2-acylamino-1-(3- or 4-carboxyphenyl) benzamides 8-19 bearing C6, C8, C10, C12, C14, and C16 acyl chains at the 2-amino position of 2-aminobenzoic acid. Enzyme inhibition of these compounds was investigated using in vitro PCAF HAT assays. The inhibitory activities of compounds 8-10, 16, and 19 were similar to that of anacardic acid, and 17 was found to be more active than anacardic acid at 100 μM. Compounds 11-15 showed the low inhibitory activity on PCAF HAT. The cytotoxicity of the synthesized compounds was evaluated by SRB (sulforhodamine B) assay against seven human cancer cell lines: HT-29 (colon), HCT-116 (colon), MDA-231 (breast), A549 (lung), Hep3B (hepatoma), HeLa (cervical) and Caki (kidney) and one normal cell line (HSF). Compound 17 was more active than anacardic acid against human colon cancer (HCT 116, IC50: 29.17 μM), human lung cancer (A549, IC 50: 32.09 μM) cell lines. 18 was more active than anacardic acid against human colon cancer (HT-29, IC50: 35.49 μM and HCT 116, IC50: 27.56 μM), human lung cancer (A549, IC50: 30.69 μM), and human cervical cancer (HeLa, IC50: 34.41 μM) cell lines. The apparent permeability coefficient (Papp, cm/s) values of two compounds (16 and 17) were evaluated as 68.21 and 71.48 × 10 -6 cm/s by Caco-2 cell permeability assay.
