19820-56-5Relevant articles and documents
A comparative experimental and theoretical investigation of hydrogen-bond, halogen-bond and π-π interactions in the solid-state supramolecular assembly of 2- and 4-formylphenyl arylsulfonates
Andleeb, Hina,Khan, Imtiaz,Bauzá, Antonio,Tahir, Muhammad Nawaz,Simpson, Jim,Hameed, Shahid,Frontera, Antonio
, p. 816 - 829 (2018)
To explore the operational role of noncovalent interactions in supramolecular architectures with designed topologies, a series of solid-state structures of 2- and 4-formylphenyl 4-substituted benzenesulfonates was investigated. The compounds are 2-formylp
Synthesis of (1,3,4-thiadiazol-2-yl)-acrylamide derivatives as potential antitumor agents against acute leukemia cells
An, Ran,Guo, Chun,Li, Qing,Li, Yan,Wang, Renxiao,Xu, Yaochun,Zhou, Mi
supporting information, (2020/03/25)
A lead compound with the (1,3,4-thiadiazol-2-yl)-acrylamide scaffold was discovered to have significant cytotoxicity on several tumor cell lines in an in-house cell-based screening. A total of 60 derivative compounds were then synthesized and tested in a CCK-8 cell viability assay. Some of them exhibited improved cytotoxic activities. The most potent compounds had IC50 values of 1–5 μM on two acute leukemia tumor cell lines, i.e. RS4;11 and HL-60. Flow cytometry analysis of several active compounds and detection of caspase activation indicated that they induced caspase-dependent apoptosis. It was also encouraging to observe that these compounds did not have obvious cytotoxicity on normal cells, i.e. IC50 > 50 μM on HEK-293T cells. Although the molecular targets of this class of compound are yet to be revealed, our current results suggest that this class of compound represents a new possibility for developing drug candidates against acute leukemia.
Thiazole amide compound and preparation method, pharmaceutical composition and application thereof
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Paragraph 0207; 0229; 0230; 0231, (2019/01/08)
The invention discloses a thiazole amide compound and a preparation method thereof, a pharmaceutical composition and application thereof. The thiazole amide compound as shown in a formula I and a pharmaceutically acceptable salt thereof are provided, and
Concise approach to mono- And disubstituted luotonin A analogs and their cytotoxicity test
Kagawa, Natsuko,Nishimura, Kimiko,Abe, Shinya,Masuko, Takashi,Toyota, Masahiro
, p. 514 - 522 (2019/07/31)
A concise approach for the preparation of luotonin A analogs has been developed. The new synthetic route contains an anion-assisted intramolecular double hetero Diels Alder reaction and a direct oxidative cross coupling reaction. Some synthetic luotonin A analogs show cytotoxic activities against Daudi and Jurkat human cancer cells as potent as camptothecin.
One-Pot Multicomponent Synthesis of Novel 2-Tosyloxyphenylpyrans under Green and Conventional Condition with Anti-inflammatory Activity
Khodairy, Ahmed,Ali, Ali M.,Aboelez, Moustafa O.,El-Wassimy
, p. 1442 - 1449 (2017/03/27)
A mild, efficient, and environmentally green protocol for the synthesis of 2-tosyloxyphenylpyran derivatives 3, 4, 5, 6, 7, 8, 9, 10, 11 via reaction of 2-tosyloxybenzaldehyde (1) with malononitrile and some ketonic reagents in one-pot, three component re
Asymmetric addition of phenylacetylene to aldehydes catalyzed by complex of O-sulfonyl camphor derivatives and titanium
Lee, Dong-Sheng,Gau, Chang-Weu,Chen, Yu-Yang,Lu, Ta-Jung
, p. 242 - 246 (2016/04/05)
Several novel ligands that are based on the camphor skeleton or contain the O-sulfonyl group were synthesized and used in the asymmetric addition of phenylacetylene to aldehydes. This enantioselective reaction afforded chiral propargylic alcohols in high
Access to phthalazinones via palladium-catalyzed three-component cycloamino-carbonylation of 2-formylaryl tosylates, hydrazines and CO
Liu, Bin,Zhang, Chunlei,Zhou, Xigeng
supporting information, p. 8282 - 8286 (2016/12/02)
The palladium-catalyzed three-component cycloaminocarbonylation of 2-formylaryl tosylates with hydrazines and carbon monoxide has been established, which provides an efficient method for synthesis of substituted phthalazinones. In addition, by applying this protocol as the key step, Hydralazine can easily be synthesized in 65% yield.
Coordinating effect in ring-opening polymerization of ε-caprolactone using aluminum complexes bearing bisphenolate as catalysts
Chen, Hsing-Yin,Lee, Ying-Hsien,Chiang, Michael Y.,Lu, Wei-Yi,Tseng, Hsi-Ching,Tsai, Hsin-Yi,Chen, Yu-Hsieh,Lai, Yi-Chun,Chen, Hsuan-Ying
, p. 82018 - 82026 (2015/10/12)
A series of Al complexes bearing diphenolate ligands was synthesized and their application for the ring-opening polymerization of ε-caprolactone was studied. Positional variation of the substituent on the aryl ring of the RCH(4,6-di-t-butylphenol)2 ligand was shown to have a considerable influence on the catalysis result. Complexes with a ortho-substituent showed greater catalytic activity than those with a para-substituent. Substitutions of an aryl moiety by H or methyl groups resulted in the catalytic activity falling between that of the ortho-substitution Al complexes and that of the para ones. Our results demonstrate that the coordinated functional group in the ortho-position of the phenyl ring could increase the catalytic activity. Moreover, X-rays of the structure and DFT analysis revealed that the coordinated functional group in the ortho-position could bridge two Al centers resulting in the transformation of a dinuclear Al complex with bridging benzyl alkoxide into a complex with terminal benzyl alkoxide, further promoting the efficacy of the initiator.
Synthesis and antiproliferative evaluation of 2'-arenesulfonyloxy-5- benzylidene-thiazolidine-2,4-diones
Chen, Emily M.,Lu, Pei-Jung,Shaw, Arthur Y.
, p. 792 - 798 (2012/10/29)
A series of 2'-arenesulfonyloxy-5-benzylidene-thiazolidine-2,4-diones (TZDs) were synthesized and examined for their antiproliferative effects on a panel of carcinoma cell lines. Our results indicated that initial synthesis of 5-[2'-hydroxybenzylidene]-2,
Synthesis, characterization and structures of 2-(3,5-dimethylpyrazol-1-yl) ethylseleno derivatives and their probable glutathione peroxidase (GPx) like activity
Hodage, Ananda S.,Phadnis, Prasad P.,Wadawale, Amey,Priyadarsini,Jain, Vimal K.
supporting information; experimental part, p. 2992 - 2998 (2011/06/16)
A series of 2-(3,5-dimethylpyrazol-1-yl)ethylseleno derivatives has been synthesized. The glutathione peroxidase like catalytic activity of these compounds has been studied in a model system, in which reduction of hydrogen peroxide with dithiothreitol (DTTred), in the presence of an organoselenium compound was investigated by 1H NMR spectroscopy. All these compounds exhibit GPx like catalytic activities and the catalytic reaction proceeds through a selenoxide intermediate, identified by 77Se{ 1H} NMR spectroscopy.