ChemInform Abstract: Synthesis of Some New Pyrazole and Pyrimidine Derivatives Carrying a Sulfonamide Moiety of Expected Antitumor Activity and Study of the Synergistic Effect of γ-Irradiation.

ChemInform ◽  
2010 ◽  
Vol 41 (33) ◽  
pp. no-no
Author(s):  
Mostafa M. Ghorab ◽  
Fatma A. Ragab ◽  
Helmy I. Heiba ◽  
Hanan A. Youssef ◽  
Marwa Galal
Keyword(s):  
Antitumor Activity ◽  
Synergistic Effect ◽  
Pyrimidine Derivatives ◽  
Γ Irradiation

Synthesis of Some New Tetracyclic Pyrimidine Derivatives Using Exocyclic α,β-Unsaturated Ketone and Evaluation of Their Antitumor Activities

2016 ◽  
Vol 12 (8) ◽  
pp. 311-317
Author(s):  
Kamelia El-Mahdy
Keyword(s):  
Antitumor Activity ◽  
Spectroscopic Data ◽  
Acid Hydrazide ◽  
Chloroacetic Acid ◽  
Equimolar Amount ◽  
Unsaturated Ketone ◽  
Cyanoacetic Acid ◽  
Antitumor Activities ◽  
Pyrimidine Derivatives ◽  
Cyanoacetic Acid Hydrazide

Thiazolopyrimidine 2 was obtained from the reaction of dihydropyrimidinone with chloroacetic acid and benzaldehyde. Thiazolopyrimidine 2 containing an α,β-unsaturated ketonic function [-CH=CH-CO-] has been used as a component of Michael addition with an equimolar amount of dinucleophiles to give a series of novel tetracyclic pyrimidine derivatives. Treatment of thiazolopyrimidine 2 with uracil, aminotriazole, cyanoacetic acid hydrazide, o-phenylenediamine or diaminopyridine afforded the corresponding pyridopyrimidine, triazolopyrimidine, pyrazolone, benzodiazepine and triazepine derivative, respectively. The detailed synthesis, spectroscopic data, and antitumor activity for synthesized compounds were reported.

scholarly journals Co-delivery of doxorubicin, docosahexaenoic acid, and α-tocopherol succinate by nanostructured lipid carriers has a synergistic effect to enhance antitumor activity and reduce toxicity

2020 ◽  
Vol 132 ◽  
pp. 110876
Author(s):  
Eduardo Burgarelli Lages ◽  
Renata Salgado Fernandes ◽  
Juliana de Oliveira Silva ◽  
Ângelo Malachias de Souza ◽  
Geovanni Dantas Cassali ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Docosahexaenoic Acid ◽  
Synergistic Effect ◽  
Nanostructured Lipid Carriers

Targeting the immunosuppressive tumor microenvironment: Synergistic effect of low-dose IL12 in combination with dual immune checkpoint inhibition in a preclinical model of ovarian cancer.

2020 ◽  
Vol 38 (5_suppl) ◽  
pp. 7-7
Author(s):  
Paul G. Pavicic ◽  
Patricia A. Rayman ◽  
Hussein Al-Sudani ◽  
C. Marcela Diaz-Montero ◽  
Haider Mahdi
Keyword(s):  
Ovarian Cancer ◽  
T Cells ◽  
Tumor Microenvironment ◽  
Antitumor Activity ◽  
Synergistic Effect ◽  
Immune Checkpoint ◽  
Low Dose ◽  
Checkpoint Inhibition ◽  
Immune Checkpoint Inhibition ◽  
Activated T Cells

7 Background: Epithelial ovarian cancer (OC) is the most lethal gynecologic cancer with ~22,000 women diagnosed annually in the US. The impact of immune checkpoint inhibition (ICI) in the treatment of solid tumors has been significant. However, the response rates for OC are low ranging from 11-15%. It is critical to explore strategies to enhance the efficacy of ICI immunotherapy in OC. Targeting immunosuppressive factors and cells within the tumor microenvironment (TME) represents a feasible approach. The use of IL12 is attractive because induces potent antitumor activity by targeting myeloid cells and lymphocytes. However its clinical application has been hindered by its potential systemic toxicity. Here we explore the use of low dose intraperitoneal IL12 to enhance the antitumor activity of dual ICI in OC. Methods: Mice bearing ID8-VEGF tumors implanted intraperitoneally received either anti-PD1 alone or dual ICI treatment of anti-PD1 plus anti-CTLA4 with or without low dose IL12. Ascites accumulation was used as surrogate for tumor progression and determined by assessing weight increase. Blood and ascites were analyzed by flow cytometry for frequency of PMN-MDSC, M-MDSC, and activated T cells. Results: Low dose IL12 alone induced a significant delay in ascites accumulation when compared to untreated controls or mice treated with PD1 monotherapy or dual ICI. Addition of IL12 to dual ICI resulted in significant tumor regression and extended survival benefit compared to dual ICI alone. A synergistic effect of IL12 was not observed when combined with PD1 monotherapy. Antitumor responses associated with a marked decrease in the frequency of M-MDSC in blood and a decrease in both PMN- and M-MDSC in ascites. Decrease in MDSC associated with elevated levels of activated T cells. Conclusions: Low dose IL12 can induce regression of ID8-VEGF tumors. However, durable responses were only observed when IL12 was added to dual ICI. This suggests that IL12 can induce changes in the TME, particularly on MDSC, that can potentiate the antitumor activity of dual ICI. Our findings also suggest a crucial role of CTLA4 blockade perhaps via Treg targeting.

ChemInform Abstract: PYRIMIDINE DERIVATIVES. XLIV. SOME 5,6-DIHYDROURACILS AND THIOURACILS AND STUDY OF THEIR ANTITUMOR ACTIVITY

1977 ◽  
Vol 8 (28) ◽  
pp. no-no
Author(s):  
M. A. KALDRIKYAN ◽  
V. A. GEBOYAN ◽  
F. G. ARSENYAN ◽  
B. T. GARIBDZHANYAN ◽  
A. A. AROYAN
Keyword(s):  
Antitumor Activity ◽  
Pyrimidine Derivatives

Synthesis and antitumor activity of pyrido [2,3-d]pyrimidine and pyrido[2,3-d] [1,2,4]triazolo[4,3-a]pyrimidine derivatives that induce apoptosis through G1 cell-cycle arrest

2014 ◽  
Vol 83 ◽  
pp. 155-166 ◽  
Author(s):  
Mohamed Fares ◽  
Sahar Mahmoud Abou-Seri ◽  
Hatem A. Abdel-Aziz ◽  
Safinaz E.-S. Abbas ◽  
Mohieldin Magdy Youssef ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Antitumor Activity ◽  
Cell Cycle Arrest ◽  
Pyrimidine Derivatives ◽  
Cycle Arrest ◽  
G1 Cell Cycle Arrest

Pyrimidine derivatives. XLIX. Some derivatives of the 2-substituted phenoxymethyl-4-hydroxy-6-methylpyrimidines and the study of their antitumor activity

1978 ◽  
Vol 12 (5) ◽  
pp. 620-625
Author(s):  
M. S. Kramer ◽  
A. G. Saakyan ◽  
B. T. Garibdzhanyan ◽  
G. M. Stepanyan ◽  
R. G. Mirzoyan ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Pyrimidine Derivatives ◽  
Derivatives Of

scholarly journals Synergistic effect of gamma (γ)-irradiation and microencapsulated antimicrobials against Listeria monocytogenes on ready-to-eat (RTE) meat

2015 ◽  
Vol 46 ◽  
pp. 507-514 ◽  
Author(s):  
Tanzina Huq ◽  
Khanh Dang Vu ◽  
Bernard Riedl ◽  
Jean Bouchard ◽  
Monique Lacroix
Keyword(s):  
Listeria Monocytogenes ◽  
Synergistic Effect ◽  
Γ Irradiation
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