scholarly journals Diastereoselective reduction of the tricarbonyl moiety in bicyclic tetramates giving pyroglutamates

2018 ◽  
Vol 16 (15) ◽  
pp. 2705-2710 ◽  
Author(s):  
Laia Josa-Culleré ◽  
Kirsten E. Christensen ◽  
Mark G. Moloney
Keyword(s):  
Antibacterial Activity ◽  
Small Molecules ◽  
Cell Line ◽  
Cancer Cell ◽  
Inhibitory Activity ◽  
Cancer Cell Line ◽  
Stereoselective Reduction ◽  
Weinreb Amide ◽  
Tetramic Acids ◽  
Diastereoselective Reduction

The formation of densely functionalised bicyclic tetramic acids by both stereoselective reduction and Grignard displacement of a Weinreb amide gives bioactive small molecules, with antibacterial activity along with some cancer-cell line inhibitory activity.

scholarly journals IN VITRO CYTOTOXIC ACTIVITY OF SECOISOLARICIRESINOL DIGLUCOSIDE ON HT-29, PA-1 CELL LINES, AND α-AMYLASE INHIBITORY ACTIVITY

2019 ◽  
pp. 168-173
Author(s):  
GUNABHUSHANA DADDALA ◽  
SWAROOPARANI A
Keyword(s):  
Cytotoxic Activity ◽  
Cell Line ◽  
Cancer Cell ◽  
Inhibitory Activity ◽  
Ovarian Cancer Cell Line ◽  
Cancer Cell Line ◽  
Secoisolariciresinol Diglucoside ◽  
Human Colon Cancer ◽  
Ht 29

Objective: The present study was conducted to evaluate the in vitro cytotoxic activity and α- amylase inhibitory activity of secoisolariciresinol diglucoside (SDG). Methods: The cytotoxic activity was conducted on HT-29 (human colon cancer cell line) and PA-1 (human ovarian cancer cell line) by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay and the α- amylase inhibitory activity using acarbose as a standard. Both the tests were evaluated at different concentrations, 3.125–100 μg/ml and 50–2000 μg correspondingly and the concentration required for a 50% inhibition of viability (IC50) was determined graphically. The effect of the samples on the proliferation of HT-29 and PA-1 was expressed as the percentage cell viability. Results: SDG exhibited a considerable dose- and time-dependent inhibition on both HT-29 and PA-1 and also observed a concentration-dependent α-amylase inhibitory activity that leads in reduction of starch hydrolysis and hence eventually to lowered glucose levels. Conclusion: The present in vitro study concluded that SDG can be a potent anticancer and moderate hyperglycemic component.

Synthesis of Novel Thieno[2,3-d]pyrimidine Derivatives and Evaluation of Their Cytotoxicity and EGFR Inhibitory Activity

2018 ◽  
Vol 18 (5) ◽  
pp. 747-756 ◽  
Author(s):  
Mina E. Adly ◽  
Ehab M. Gedawy ◽  
Afaf A. El-Malah ◽  
Farag A. El-Telbany
Keyword(s):  
Single Dose ◽  
Cytotoxic Activity ◽  
Cell Line ◽  
Cancer Cell ◽  
Inhibitory Activity ◽  
Cancer Biology ◽  
Human Tumor ◽  
Cancer Cell Line ◽  
Pyrimidine Derivatives ◽  
Comparable Activity

Background: 4-Substitutedaminoquinazoline scaffolds were reported to possess potent cytotoxic and EGFR inhibitory activity such as gefitinib (Iressa), erlotinib (Tarceva) and tandutinib. Objective: Synthesis of novel 4-substitutedaminothieno[2,3-d]pyrimidine derivatives as bioisosters of 4-substitutedaminoquinazoline derivatives with potential cytotoxic and EGFR inhibitory activity. Methods: Novel 4-substitutedaminothieno[2,3-d]pyrimidine derivatives 4a-i and 5a-c were synthesized via reacting corresponding 4-chlorothieno[2,3-d]pyrimidine derivatives 3a-c with N-methylpiperazine, morpholine, N-phenylpiperazine or 1,3-propanediamine. Six compounds (2a, 4d, 4e, 5a-c) were selected by the National Cancer Institute (USA) for evaluating their cytotoxic activity using 60 different human tumor cell lines using a single dose (10-5 Molar). The rest of the synthesized compounds (2b, 2c, 3a-c, 4a-c and 4f-i) were subjected to screening against T47D breast cancer cell line using a single dose (10-5 Molar) at Pharmacology lab., Cancer biology lab., Egyptian National Institute. Moreover, compounds 2a and 4b-e were subjected to further evaluation by IC50 determination. Finally, the inhibition of epidermal growth factor receptor (EGFR) was then investigated for the most active compounds 2a and 4d. Results: Compounds 2a and 4b-e showed significant cytotoxic activity. Compound 2a was more potent than doxorubicin against lung cancer cell line A549 with IC50 = 13.40 μM and comparable activity against MCF7. Compound 4d exhibited more potent activity than Doxorubicin against prostate PC3 (IC50 = 14.13 µM) while showed comparable activity against MCF7 and T47D. Conclusion: 4-Substitutedaminothieno[2,3-d]pyrimidine is a promising backbone for the design and synthesis of potent cytotoxic leads.

scholarly journals A New Chromene Isolated from Ageratum conyzoides

2011 ◽  
Vol 6 (9) ◽  
pp. 1934578X1100600 ◽  
Author(s):  
Abiodun Humphrey Adebayo ◽  
Chang-Jiu Ji ◽  
Yu-Mei Zhang ◽  
Wen-Jun He ◽  
Guang-Zhi Zeng ◽  
...  
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Inhibitory Activity ◽  
Cancer Cell Line ◽  
Ethanol Extract ◽  
2D Nmr ◽  
Ageratum Conyzoides ◽  
2D Nmr Spectroscopy ◽  
Whole Plant ◽  
First Time

From the ethanol extract of the whole plant of Ageratum conyzoides L. (Compositae), one new chromene, 2,2-dimethylchromene 7-methoxy-6- O-β-D-glucopyranoside, was isolated, together with thirteen known compounds, seven of which were being reported for the first time. The compounds were all characterized by MS, IR, 1D- and 2D-NMR spectroscopy. 7,3′,5′-Tri- O-methyltricetin (7), precocene II (9), 3,5,7,4′-tetrahydroxyflavone (13) and 5,6,7,3′,4′,5′-hexamethoxyflavone (14) exhibited inhibitory activity on the P-388 cancer cell line with IC50 values of 12.8, 24.8, 3.5 and 7.8 μM respectively, while compound 9 exhibited inhibitory activity on the HT-29 cancer cell line with an IC50 value of 61μM; the others showed no significant cytotoxic activity on the cell lines tested.

scholarly journals Evaluating the Inhibitory Activity of Apigenin Extracted from Salvia officinalis leaves on the Growth of L20B Cancer Cell Line

2012 ◽  
Vol 9 (2) ◽  
pp. 194-199
Author(s):  
Baghdad Science Journal
Keyword(s):  
Carbon Tetrachloride ◽  
Vitamin C ◽  
Cell Line ◽  
Cancer Cell ◽  
Inhibitory Activity ◽  
Cancer Cell Line ◽  
Salvia Officinalis ◽  
Low Concentrations ◽  
Incubation Periods

The study aimed to evaluating the inhibitory activity of apigenin extracted from Salvia officinalis leaves on the growth of L20B cancer cell in vitro, and through two incubation periods; 48 and 72 hours. Accordingly, eight concentrations (1.56, 3.13, 6.25, 12.5, 25.0, 50.0, 100.0 and 200.0 micromol) of apigenin and similar concentrations of vitamin C and carbon tetrachloride (CCl4) were tested. The apigenin revealed its significant inhibitory potentials against the growth of L20B cell line, especially at the low concentrations (1.56, 3.13 and 6.25 micromol) and at 72 incubation period in comparison with vitamin C and CCl4.

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