74470-32-9Relevant articles and documents
Triazolothiadizepinylquinolines as potential MetAP-2 and NMT inhibitors: Microwave-assisted synthesis, pharmacological evaluation and molecular docking studies
Shaikh, Saba Kauser J.,Kamble, Ravindra R.,Bayannavar, Praveen K.,Somagond, Shilpa M.,Joshi, Shrinivas D.
, (2019/12/11)
The enzymes MetAP-2 and NMT play a crucial role in the process of myristoylation of oncoproteins which is deregulated in many types of cancers. Execution of both these enzymes is considered as strategy for the intervention of various cancers and relative fungal infections, and hence the discovery of novel MetAP-2 and NMT inhibitors necessitate their high relevancy. In this investigation, we have synthesized a series of novel seven-membered triazolothiadiazepinyl quinolines 10(a–m) distinctively under microwave irradiation technique and identified as selective MetAP-2 and NMT inhibitors. Amongst the functionalized derivatives when evaluated for the in vitro antifungal assay, compounds 10b, 10c, 10e and 10f were considered promising due to notable inhibitory effects (MIC = 0.2 mg/mL) on Aspergillus fumigatus. Screening of the anticancer activity against NCI-60 Human tumor cell lines portrayed that conjugates 10b, 10c, 10e and 10f were found to be moderately effective against the Renal Cancer cell line UO-31. The data acquired from biological studies was further validated by molecular docking studies and pharmacokinetic evaluation.
Nitrogen-containing fatty alcohol ester barium salt, and preparation method, composition and application thereof
-
Paragraph 0029-0032, (2019/10/01)
The invention discloses a nitrogen-containing fatty alcohol ester barium salt, and a preparation method, a composition and an application thereof. The chemical formula of the nitrogen-containing fattyalcohol ester barium salt is Ba(C7H3O2NSR)2, and R is a C12-20 alkyl group. The barium salt belongs to a mercaptide, can act as an antioxidant, and can significantly improve the long-acting stabilityof PVC. The barium salt of the invention contains the nitrogen atom, a stabilizer formed by combining the barium salt with a nitrogen-containing zinc salt and an auxiliary stabilizer can obviously improve the thermal stability of the PVC, and the nitrogen-containing zinc has higher activity than common zinc carboxylate, and can fast absorb allyl chloride, significantly improve initial dyeing andprolong later zinc burning.
INDOLE DERIVATIVES AS LIGANDS OF CRTH2 RECEPTORS
-
Page/Page column 24, (2010/12/29)
The following compounds are CRTH2 antagonists, useful in treatment of respiratory disease: {3-[3-chloro-4-(pyridine-2-sulfonyl)isothiazol-5-ylmethyl]-5-fluoro-2- methylindol-1-yl}acetic acid, [3-(5-benzenesulfonyl-3-methyl-3H-imidazol-4-ylmethyl)-5-fluoro