25642-37-9Relevant academic research and scientific papers
Palladium(II) N^O Chelating Complexes Catalyzed One-Pot Approach for Synthesis of Quinazolin-4(3 H)-ones via Acceptorless Dehydrogenative Coupling of Benzyl Alcohols and 2-Aminobenzamide
Balaji, Sundarraman,Balamurugan, Gunasekaran,Ramesh, Rengan,Semeril, David
, p. 725 - 734 (2021/04/06)
A convenient protocol for the one-pot synthesis of quinazolin-4(3H)-ones using palladium(II) complexes via dehydrogenative coupling of readily available benzyl alcohols and 2-aminobenzamide has been described. New structurally related Pd(II) N^O chelating complexes of general configuration [Pd(L)Cl(PPh3)] (where L = dimethylamino benzoylhydrazone ligands) have been designed and synthesized. The formation of the complexes has been recognized by analytical and spectral methods (FT-IR, NMR, HR-MS). The presence of a square-planar geometry around the palladium(II) ion was confirmed by single crystal X-ray diffraction study. A wide range of substituted quinazolinones have been successfully achieved from a diverse range of benzyl alcohols in good to excellent yields using 1.0 mol % of catalyst loading under aerobic conditions. Furthermore, control experiments reveal that the dehydrogenative coupling reaction involves initially the formation of an aldehyde intermediate and subsequent formation of a cyclic aminal intermediate.
Organic boron photosensitizer based on aggregation-induced emission, and application thereof in treatment of multi-drug-resistant bacterium infection
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Paragraph 0084-0087, (2021/08/07)
The invention relates to an organic boron photosensitizer based on aggregation-induced emission, a preparation method thereof and application of the organic boron photosensitizer in photodynamic therapy for multi-drug-resistant bacterium infection. A seri
Synthesis and Structure of Arene Ru(II) NΛO-Chelating Complexes: In Vitro Cytotoxicity and Cancer Cell Death Mechanism
Balaji, Sundarraman,Mohamed Subarkhan, Mohamed Kasim,Ramesh, Rengan,Wang, Hangxiang,Semeril, David
, p. 1366 - 1375 (2020/04/20)
A panel of six new structurally related organometallic arene Ru(II) complexes of general composition [(η6-benzene)Ru(L)Cl] (1-3) and [(η6-p-cymene)Ru(L)Cl] (4-6) (L = dimethylaminobenzhydrazones) have been designed and synthesized in search of new rutheni
Organoboron compound based on acyl hydrazone ligand and preparation method and application thereof
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Paragraph 0086-0088, (2019/12/08)
The invention relates to an organoboron compound based on an acyl hydrazone ligand and a preparation method and an application thereof. A series of organoboron fluorescent compounds based on acyl hydrazone ligands synthesized by the invention are easy to
Synthesis, biological evaluation, drug-likeness, and in silico screening of novel benzylidene-hydrazone analogues as small molecule anticancer agents
Alam, Mohammad Sayed,Lee, Dong-Ung
, p. 191 - 201 (2016/03/12)
A series of fifteen benzylidene-hydrazone analogues (3a-o), including eight new compounds, were synthesized and evaluated for their cytotoxic activities in four human cancer cell lines and for their antioxidant activities using DPPH. Of the tested compounds 3e, which possesses two methoxy substituents in its benzylidene phenyl ring, was found to be potently cytotoxic to all cancer cell lines tested with IC50 values of 0.12 (lung), 0.024 (ovarian), 0.097 (melanoma), and 0.05 μM (colon), and these IC50 values were comparable to those of the doxorubicin standard (IC50 = 0.021, 0.074, 0.001, and 0.872 μM, respectively). DPPH assay showed compounds 3f, 3i, and 3g had IC50 values of 0.60, 0.99, and 1.30 μM, respectively, which were comparable to that of ascorbic acid (IC50 = 0.87 μM). Computational parameters such as, drug-likeness, ADME properties, toxicity effects, and drug scores were evaluated, and none of the fifteen compounds violated Lipinski's rule of five or Veber's rule, and thus they demonstrated good drug-likeness properties. In addition, all fifteen compounds had a higher drug score than the doxorubicin and BIBR1532. In silico screening was also conducted by docking of the active compounds on the active site of telomerase reverse transcriptase catalytic subunit, an important therapeutic target of anticancer agents, to determine the probable binding properties. The total binding energies of docked compounds are correlated well with cytotoxic potencies (pIC50) against lung, ovarian, melanoma, and colon cancer cell lines indicating that the benzylidene-hydrazones could use for the development of new anticancer agents as a telomerase inhibitor.
3-Acetyl-2,5-diaryl-2,3-dihydro-1,3,4-oxadiazoles: A new scaffold for the selective inhibition of monoamine oxidase B
MacCioni, Elias,Alcaro, Stefano,Cirilli, Roberto,Vigo, Sara,Cardia, Maria Cristina,Sanna, Maria Luisa,Meleddu, Rita,Yanez, Matilde,Costa, Giosuè,Casu, Laura,Matyus, Peter,Distinto, Simona
experimental part, p. 6394 - 6398 (2011/11/06)
3-Acetyl-2,5-diaryl-2,3-dihydro-1,3,4-oxadiazoles were designed, synthesized, and tested as inhibitors against human monoamine oxidase (MAO) A and B isoforms. Several compounds, obtained as racemates, were identified as selective MAO-B inhibitors. The enantiomers of some derivatives were separated by enantioselective HPLC and tested. The R-enantiomers always showed the highest activity. Docking study and molecular dynamic simulations demonstrated the putative binding mode. We conclude that these 1,3,4-oxadiazoles derivatives are promising reversible and selective MAO-B inhibitors.
