89756-60-5Relevant articles and documents
Design, synthesis, cytotoxic activity, and apoptosis inducing effects of 4- And N-substituted benzoyltaurinamide derivatives
Akgül, ?zlem,Erdo?an, Mümin Alper,Birim, Dervi?,Kayaba?i, ?a?la,Gündüz, Cumhur,Arma?an, Güliz
, p. 1674 - 1693 (2021/01/05)
In this study, a group of 4-substituted benzoyltaurinamide derivatives were designed, synthesized, and investigated for their anticancer activity against three cancer cell lines and one nontumorigenic cell line by MTT assay. Among the final compounds, methoxyphenyl derivatives 14, 15, 16 were found to be effective against all the tested cancerous cell lines with promising selectivity. The most active compounds were further evaluated to determine the molecular mechanism of their anticancer activity by using western blot assay and the Annexin V-FITC/PI test. Compound 14 (in SH-SY5Y and MDA-MB-231 cell lines) and 15 (in SH-SY5Y cell line) were found to induce intrinsic apoptotic pathway by upregulating BAX, caspase-3, and caspase-9, while downregulating Bcl-2 and Bcl-xL expression levels. According to mechanistic studies, compounds displayed their anticancer activity via three different mechanisms: a. caspase-dependent, b. caspase-independent, and c. caspase-dependent pathway that excluded caspase-9 activation. As a result, this study provides interesting data which can be used to design new taurine-based anticancer derivatives.
Method for synthesis of taurideamide hydrochloride (2-aminoethylsulfonamide hydrochloride)
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Paragraph 0032; 0057, (2018/04/02)
The present invention discloses a method for synthesis of taurideamide hydrochloride (2-aminoethylsulfonamide hydrochloride) which is an important basic medicinal raw material, the preparation methodof the taurideamide hydrochloride (2-aminoethylsulfonamide hydrochloride) belongs to the field of medicinal chemistry synthesis. Compound (I) (2-bromoethylsulfonyl chloride) is used as a starting material, ammonia is used as a nucleophilic reagent for nucleophilic substitution of chlorine atoms on sulfonyl chloride and bromine atoms on 2-site of ethyl of the compound (I) (2-bromoethylsulfonyl chloride), and the compound (II) taurideamide hydrochloride (2-aminoethylsulfonamide hydrochloride) is formed by action of the compound (I) (2-bromoethylsulfonyl chloride) and hydrochloric acid in ethanol, and a reaction scheme is shown in the specification. The method has the advantages of simple route, simple post-treatment, little side reaction and high yield, and meets the requirements of industrialized production.
ESTRA-1,3,5(10),16-TETRAENE-3-CARBOXAMIDES FOR INHIBITION OF 17Β-HYDROXYSTEROID DEHYDROGENASE (AKR1 C3)
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, (2016/02/18)
The invention relates to AKR1C3 inhibitors of formula (I) and to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of bleeding disorders and endometriosis.