A Novel Route to Isoquinoline[2,1-g][1,6]naphthyridine, Pyrazolo[5,1-a] isoquinoline and Pyridazino[4´,5´:3,4]pyrazolo[5,1-a]isoquinoline Derivatives With Evaluation of Antitumor Activities

2013 ◽  
Vol 68 (8) ◽  
pp. 895-904 ◽  
Author(s):  
Hamdi M. Hassaneen ◽  
Wagnat W. Wardkhan ◽  
Yasmin Sh. Mohammed
Keyword(s):  
Sodium Azide ◽  
Sodium Dithionite ◽  
Phenyl Isothiocyanate ◽  
Antitumor Activities ◽  
Isoquinoline Derivatives ◽  
Isoquinoline Derivative

(E)-2-Chloro-3-(2-cyanovinyl)-9,10-dimethoxy-4-oxo-6,7-dihydro-4H-pyrido[2,1-a] isoquinoline- 1-carbonitrile (5) was obtained by treatment of the 2-chloro-3-formylpyrido[2,1-a]isoquinoline derivative 3 with 2-(triphenylphosphoranylidene)acetonitrile (4). Treatment of 5 with sodium azide afforded the corresponding azido compound 6 which could be reduced by sodium dithionite to compound 7. A novel isoquinolino[2,1-g][1,6]naphthyridine derivative 11 was obtained by the reaction of phenyl isothiocyanate with the phosphorane compound 8, which was prepared by the reaction of compound 6 with triphenylphosphine. Treatment of 5 with amines 12a-c and thiophenols 14a-c in refluxing ethanol afforded the corresponding substitution products 13a-c and 15a-c, respectively. Also, the reaction of 1 with a-oxo hydroxamoyl chlorides 16 was reinvestigated, and the synthesized pyrazoloisoquinolines 19a-f and pyridazinopyrazoloisoquinolines 20a, e were screened for their in vitro antitumor activities.

Synthesis and Antitumor Activity Evaluation of New Phenanthrene-Based Tylophorine Derivatives

2019 ◽  
Vol 16 (6) ◽  
pp. 462-467
Author(s):  
Songtao Li ◽  
Hongling Zhao ◽  
Zhifeng Yin ◽  
Shuhua Deng ◽  
Yang Gao ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Cell Lines ◽  
Antitumor Activities ◽  
Human Carcinoma ◽  
Carcinoma Cell Lines ◽  
Structure Activity ◽  
Human Carcinoma Cell ◽  
Ic50 Values ◽  
Relationship Of

A series of new phenanthrene-based tylophorine derivatives (PBTs) were synthesized in good yield and their structures were characterized by 1H-NMR spectroscopy and ESI MS. In vitro antitumor activity of these compounds against five human carcinoma cell lines, including HCT116 (colorectal), BGC-823 (gastric), HepG-2 (hepatic), Hela (cervical) and H460 (lung) cells, was evaluated by MTT assay. Among these PBTs, compound 6b showed the highest antitumor activities against HCT116 and HepG-2 cell lines with IC50 values of 6.1 and 6.4 μM, respectively, which were comparable to that of adriamycin hydrochloride. The structure-activity relationship of these compounds was also discussed based on the results of their antitumor activity.

In vitro absorption of bile salts by small intestine of rats and guinea pigs

1961 ◽  
Vol 200 (2) ◽  
pp. 313-317 ◽  
Author(s):  
Leon Lack ◽  
I. M. Weiner
Keyword(s):  
Small Intestine ◽  
Bile Acid ◽  
Active Transport ◽  
Sodium Azide ◽  
Concentration Gradient ◽  
Guinea Pigs ◽  
Bile Salts ◽  
Ileal Segment

The transport of taurocholic and glycocholic acids by the small intestine of rats and guinea pigs against a concentration gradient was studied by the everted gutsac technique. Transport of these substances is limited to the distal ileal segment. This transport is inhibited by anoxia, dinitrophenol and sodium azide. The system has a transport maximum. On the basis of these criteria bile acid reabsorption is considered to occur by active transport.

Sodium azide is less suitable as a positive control of drug-induced lethality for in vitro clonogenic assays

1986 ◽  
Vol 4 (4) ◽  
pp. 367-371 ◽  
Author(s):  
Peter Lelieveld ◽  
Matti S. Aapro ◽  
Rob van Lambalgen ◽  
Kor J. van den Berg
Keyword(s):  
Sodium Azide ◽  
Positive Control ◽  
Drug Induced ◽  
Clonogenic Assays

scholarly journals 8-Hydroxyquinoline-5-Sulfonic Acid-Containing Poly(Vinyl Alcohol)/Chitosan Electrospun Materials and Their Cu2+ and Fe3+ Complexes: Preparation, Antibacterial, Antifungal and Antitumor Activities

Polymers ◽  
2021 ◽  
Vol 13 (16) ◽  
pp. 2690
Author(s):  
Milena Ignatova ◽  
Nevena Manolova ◽  
Iliya Rashkov ◽  
Nadya Markova ◽  
Rositsa Kukeva ◽  
...  
Keyword(s):  
Vinyl Alcohol ◽  
Sulfonic Acid ◽  
Electron Paramagnetic Resonance Spectroscopy ◽  
Local Treatment ◽  
Poly Vinyl Alcohol ◽  
Resonance Spectroscopy ◽  
Fibrous Materials ◽  
Antitumor Activities ◽  
Antibacterial And Antifungal Activities

Novel poly(vinyl alcohol) (PVA)/chitosan (Ch)-based fibrous materials containing an ionizable model drug, 8-hydroxyquinoline-5-sulfonic acid (SQ), were successfully fabricated by electrospinning. Complexes between the components of the crosslinked PVA/Ch/SQ mats and Cu2+ and Fe3+ ions were formed. The coordination of these ions in the mats was examined by electron paramagnetic resonance spectroscopy (EPR). The microbiological screening against S. aureus and C. albicans revealed that both the incorporation of SQ in the mats and the complexation with Cu2+ and Fe3+ imparted to these materials antibacterial and antifungal activities. Moreover, the SQ-containing mats and their complexes displayed good cytotoxicity against human cervical HeLa tumor cells. The most prominent was the cytotoxicity of the Cu2+ complex of the mats. The combined antibacterial, antifungal and in vitro antitumor activities render these novel materials promising candidates for wound dressing applications and for application in the local treatment of cervical tumors.

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