3484-32-0Relevant articles and documents
Activation of the NC-H bond of Baylis-Hillman adducts of N-methylisatin with CAN/ROH
Shanmugam, Ponnusamy,Vaithiyanathan, Vadivel,Viswambharan, Baby
, p. 6851 - 6855 (2006)
A facile method for activation of the NC-H bond of N-methylisatin and Baylis-Hillman adducts of N-methylisatin with cerium ammonium nitrate (CAN) and saturated and unsaturated alcohols is reported. Adducts bearing an ester group at the activated alkene afford functionalized ethers, while those with a nitrile afforded ethers and nitrated aromatic products in good yield.
Synthesis of new spiroindolinones incorporating a benzothiazole moiety as antioxidant agents
Karali, Nilgün,Güzel, ?zlen,?zsoy, Nurten,?zbey, Süheyla,Salman, Aydin
, p. 1068 - 1077 (2010)
3H-Spiro[1,3-benzothiazole-2,3′-indol]-2′(1′H)-ones 3a-c and 4a-e were synthesized from treating the 5-substituted 1H-indole-2,3-diones with 2-aminothiophenol in ethanol. The structures were confirmed by elemental analyses, spectrometry (IR, 1H NMR, 13C NMR, HSQC-2D and LCMS-APCI) and single crystal X-ray analysis. The new compounds were screened for their antioxidant activities such as the Fe3+/ascorbate system induced inhibition of lipid peroxidation (LP) in liposomes, trolox equivalent antioxidant capacity (TEAC), scavenging effect on diphenylpicryl hydrazine (DPPH{radical dot}), and reducing power. These compounds showed potent scavenging activities against DPPH{radical dot} and 2,2′-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid) (ABTS{radical dot}+) radicals, reducing powers, and strong inhibitory capacity on lipid peroxidation. Compound 4a incorporating methyl both at R1 and R2 was found to be the most potent antioxidant described in this study. Compounds 3b and 4b were selected as representative compounds by the National Cancer Institute for screening against anticancer activity and these compounds were found to be cytotoxic against CNS cancer cell line SNB-75 in the primary screen.
BIFUNCTIONAL MOLECULES CONTAINING AN E3 UBIQUITINE LIGASE BINDING MOIETY LINKED TO A BCL6 TARGETING MOIETY
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Paragraph 00321; 00322, (2021/04/23)
Bifunctional compounds, which find utility as modulators of B-cell lymphoma 6 protein (BCL6; target protein), are described herein. In particular, the bifunctional compounds of the present disclosure contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand that binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
BCL6-targeting aromatic ring five-membered aromatic heterocyclic micromolecular organic compound and derivative and application thereof
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Paragraph 0171; 0176-0178, (2021/03/24)
The invention discloses an aromatic ring five-membered aromatic heterocyclic micromolecular organic compound or related analogues or pharmaceutically acceptable salts thereof. The structures of the compound are shown as formulas (I-IX). The invention also
