6310-45-8Relevant academic research and scientific papers
Synthesis, structure and acetylcholinesterase inhibition activity of new diarylpyrazoles
Arshad, Iqra,Dege, Necmi,Hameed, Shahid,Kharl, Aamir Ali,Nadeem, Humaira,Naseer, Muhammad Moazzam,Paracha, Rehan Zafar,Zia, Mehwash
, (2022/02/19)
A variety of diarylpyrazole derivatives III-VI were synthesized and structurally characterized using FTIR, 1H and 13C NMR spectroscopy, and in case of compound VIb by X-ray single crystal analysis. The in vitro biological studies rev
Synthesis and solid state self-assembly of a 1,4-diazepine derivative: Water cluster as molecular glue and conformational isomerism
Zia, Mehwash,Khalid, Muhammad,Hameed, Shahid,Irran, Elisabeth,Naseer, Muhammad Moazzam
, (2020/02/11)
Diazepine (a seven membered heterocycle) derivatives have emerged as “privileged structures” in chemical biology and medicinal chemistry. In this article, synthesis of a 1, 4-diazepine derivative 4 from flavone 3 in excellent yield is described. The solid state self-assembly pertaining to diazepine derivative 4 was investigated with X-ray crystallography. Fascinatingly, the solid state structure of 4 represents a remarkable example of water cluster acting as structural glue to instigate conformational isomerism and hence facilitate the crystallization process by compensating the imbalance of hydrogen-bond donors and acceptors. NBO and QTAIM based calculations show that the hydrogen-bonding network of water molecules and hyper conjugative interactions play a vital role for stabilization of structure in the solid state. To our knowledge, presented here is the first illustration of any solvent cluster stabilizing the solid-state structure in a diazepine family. In addition, the crystal structure of flavone 3 hitherto not reported is also reported.
Novel Bifunctionalization of Activated Methylene: Base-Promoted Trifluoromethylthiolation of β-Diketones with Trifluoromethanesulfinyl Chloride
Sun, Dong-Wei,Jiang, Min,Liu, Jin-Tao
, p. 10797 - 10802 (2019/07/03)
A novel bifunctionalization of activated methylene was achieved successfully through the base-promoted trifluoromethylthiolation of β-diketones or β-ketoesters with trifluoromethanesulfinyl chloride. A series of α-trifluoromethylthiolated α-chloro-β-diketones and α-chloro-β-ketoesters were obtained in moderate to good yields under mild conditions. When β-diketones containing a phenyl group with a hydroxyl or amino substituent at the ortho position were used as substrates, intramolecular trifluoromethylthiolation/cyclization reaction took place to give the corresponding cyclic products. Furthermore, the protocol could be extended to perfluoroalkylthiolation with the sodium perfluoroalkanesulfinate/POCl3 system. On the basis of experimental results, plausible mechanisms are proposed.
SYNTHESIS OF TETRACYCLIC FLAVONOIDS
-
, (2016/02/29)
The disclosure provides tetracyclic flavonoids of Formula I: and methods of making and using the same.
Synthesis and anti-cancer activities of apigenin derivatives
Zheng, Xing,Yu, Liuying,Yang, Jing,Yao, Xu,Yan, Wenna,Bo, Shaowei,Liu, Ya,Wei, Yun,Wu, Zhiyi,Wang, Guan
, p. 747 - 752 (2015/04/14)
A novel series of apigenin derivatives with phloroglucinol or resorcinol as raw materials were synthesized according to Baker-Venaktaraman reaction and their in vitro inhibitory activities on colorectal adenocarcinoma (HT-29) and leucocythemia (HL-60) cell lines were evaluated by the standard methyl thiazole tetrazolium (MTT) method. The results of biological test showed that some of apigenin derivatives possessed stronger anti-cancer activities than apigenin. Compound 6 showed the strongest activity against colorectal adenocarcinoma (HT-29) and leucocythemia (HL-60) cell lines with IC50 valure of 2.03±0.22 μM, 2.25±0.42 μM, it was better than 5-FU (12.92±0.61 μM, 9.56±0.16 μM), which shows a potezntial compound for colorectal adenocarcinoma and leucocythemia.
Synthesis, spectroscopic characterisation and X-ray analysis of regioisomeric 1,3,5-trisubstituted pyrazoles
Yunus, Uzma,Kauser, Rukhsana,Bhatti, Moazzam H.,Zia-Ul-Haq, Muhammad,Wong, Wai-Yeung
, p. 173 - 180 (2011/07/31)
A new series of regioisomeric 1,3,5-trisubstituted pyrazoles 7-9(a,b) have been synthesized by the reaction of β-diketones (4-6) with methyl hydrazine in ethanol. All the compounds are characterised by the FT-IR, 1H, 13C NMR and mass spectrometry. The crystal structure of compounds 7a, 7b and minor isomer 8b have been determined by X-ray single crystal analysis which showed either of the substituted groups attached to pyrazole ring are essentially non-planar to the central pyrazole ring. Addition of trace amounts of acetic acid during the synthesis of compound 8 resulted in an unexpected compound 10 which is characterised by the X-ray single crystal analysis and is essentially planar. However, crystal structure of 10 is already reported. All structures are further stabilized by the classic and non-classic inter- and intramolecular hydrogen bonding.
Synthesis and preliminary biological evaluation of chrysin derivatives as potential anticancer drugs
Zheng, Xing,Zhao, Fei Fei,Liu, Yun Mei,Yao, Xu,Zheng, Zi Tong,Luo, Xing,Liao, Duan Fang
scheme or table, p. 6 - 8 (2011/10/31)
A series of chrysin derivatives were prepared from 2-hydroxyacetophenone, 2,4-dihydroxyacetophenone, 2,4,6-trihydroxy- acetophenone, using modified Baker-Venkataraman transformation. Their anticancer activities in vitro were evaluated by the standard MTT method. The results of biological test showed that some of chrysin derivatives showed stronger anticancer activity than 5-fluorouracil.
N-Disubstituted carbamoyloxy flavones
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, (2008/06/13)
The invention relates to new flavone derivaties which have at least one N-disubstituted carbamoyloxy unit (OOCNR6(R7))coupled directly to one or both aromatic rings of the flavone molecule.
Synthesis and characterization of 2-(2-hydroxyphenyl)-4-aryl-1,5-benzodiazepines
Lin,Hoch
, p. 640 - 642 (2007/10/02)
Four benzodiazepine derivatives, reported earlier by other authors, were resynthesized and characterized by NMR, IR, GC/MS and elemental analysis. Three of the four compounds have melting points different from those initially reported by 35-70° C. The dif
