Potential antitumor agents. 36. Quantitative relationships between experimental antitumor activity, toxicity, and structure for the general class of 9-anilinoacridine antitumor agents

1982 ◽  
Vol 25 (3) ◽  
pp. 276-315 ◽  
Author(s):  
William A. Denny ◽  
Bruce F. Cain ◽  
Graham J. Atwell ◽  
Corwin Hansch ◽  
Augustine Panthananickal ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
General Class ◽  
Antitumor Agents ◽  
Potential Antitumor

Potential antitumor agents. 54. Chromophore requirements for in vivo antitumor activity among the general class of linear tricyclic carboxamides

1988 ◽  
Vol 31 (4) ◽  
pp. 707-712 ◽  
Author(s):  
Brian D. Palmer ◽  
Gordon W. Rewcastle ◽  
Graham J. Atwell ◽  
Bruce C. Baguley ◽  
William A. Denny
Keyword(s):  
Antitumor Activity ◽  
General Class ◽  
Antitumor Agents ◽  
In Vivo Antitumor Activity ◽  
Potential Antitumor

scholarly journals Synthesis and antitumor properties of some new 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles

2021 ◽  
pp. 37-49
Author(s):  
І. І. Мирко ◽  
Ю. І. Горак ◽  
Т. І. Чабан ◽  
І. В. Драпак ◽  
В. С. Матійчук
Keyword(s):  
Antitumor Activity ◽  
Antitumor Agents ◽  
Condensed System ◽  
Highly Active ◽  
Therapeutic Program ◽  
Composition And Structure ◽  
Antitumor Properties ◽  
High Antitumor Activity ◽  
Derivatives Of ◽  
Potential Antitumor

One of the promising methods of creating antitumor drugs is the screening of potential antitumor agents among synthesized compounds. Nitrogen-based heterocycle analogues are an extremely important class of organic substances that are widely used in medical chemistry. [1,2,4]Triazolo[3,4-b][1,3,4] thiadiazoles are among the little-studied and hard-to-reach members of this class of compounds. The aim of our work was to synthesize some new 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles, as well as the study of their antitumor activity. The objects of study were 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles. The composition and structure of the synthesized compounds were confirmed by the data of elemental analysis and 1H NMR spectroscopy. The antitumor activity of the synthesized compounds was studied in the framework of the international scientific program of the National Cancer Institute (Bethesda, Maryland, USA) DTP NCI (Developmental Therapeutic Program). The synthesis of 11 derivatives of 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles was carried out. These substances are obtained by the interaction of 5-arylfuran-2-carboxylic acids with 5-substituted 4-amino-4H-1,2,4-triazolo-3-thiols. Primary screening revealed individual 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles, which showed pronounced selective antitumor activity. The most active among the tested compounds were 3 d, 3 e and 3 j, which were further investigated during secondary screening. The results of these studies confirm the high antitumor activity of these compounds. The proposed approaches and the developed synthesis protocols made it possible to obtain a series of new 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles. The results of studies of the antitumor activity of the synthesized compounds made it possible to single out 3 highly active compounds with high antitumor activity, which gives reason to consider this condensed system as a promising molecular framework for the design of potential antitumor agents.

Synthesis and Biological Evaluation of Novel 2-imino-4-thiazolidinones as Potential Antitumor Agents for Glioblastoma

2021 ◽  
Vol 17 ◽  
Author(s):  
José Coan Campos ◽  
Patrick Teixeira Campos ◽  
Nathalia Stark Pedra ◽  
Natália Pontes Bona ◽  
Mayara Sandrielly Soares ◽  
...  
Keyword(s):  
Reactive Oxygen Species ◽  
Cell Cycle ◽  
Antitumor Activity ◽  
Cell Line ◽  
Caspase 3 ◽  
Antitumor Agents ◽  
G1 Phase ◽  
Oxygen Species ◽  
C6 Cell Line ◽  
Potential Antitumor

Aims: The purpose of our study was to explore the molecular hybridization between 2-imino-4-thizolidione and piridinic scaffolds and its potential antitumor activity. Background: Glioblastoma is the most aggressive glioma tumor clinically diagnosed malignant and highly recurrent primary brain tumor type. The standard of treatment for a glioblastoma is surgery, followed by radiation and chemotherapy using temozolomide. However, the chemoresistance has become the main barrier to treatment success. 2-imino-4-thiazolidinones are an important class of heterocyclic compounds that feature anticancer activity; however the antiglioblastoma activity is yet to be explored. Objective: To synthesize and characterize a series of novel 2-imino-4-thiazolidinones and evaluate their antiglioblastoma activity. Method: The 2-imino-4-thiazolidinone (5a-p) was synthesized according to the literature with modifications. Compounds were identified and characterized using spectroscopic analysis and X-ray diffraction. The antitumor activity was analyzed by 3-(4,5- dimethyl)-2,5-diphenyltetrazolium bromide (MTT) assay both in primary astrocyte and glioma (C6). Apoptosis and cell cycle phase were determined by flow cytometry analysis. The expression of caspase-3/7 was measured by luminescence assay. Oxidative stress parameters as: determination of reactive oxygen species (ROS), superoxide dismutase (SOD) activity, catalase (CAT) activity and total sulfhydryl content quantification were analyzed by colorimetric assays according to literature. Results: Among sixteen synthesized compounds, three displayed potent antitumor activities against tested glioblastoma cell line showed IC50 values well below the standard drug temozolomide. Therefore, compounds 5a, 5l and 5p were evaluated using cell cycle and death analysis, due to potent toxicity (2.17±1.17, 6.24±0.59, 2.93±1.12µM, respectively) in C6 cell line. The mechanism of action studies demonstrated that 5a and 5l induced apoptosis significantly increase the percentage of cells in Sub-G1 phase in the absence of necrosis. Consistent with these results, caspase-3/7 assay revealed that 5l presents pro-apoptotic activity due to the significant stimulation of caspases-3/7. Moreover, 5a, 5l and 5p increased antioxidant defense and decreased reactive oxygen species (ROS) production. Conclusion: The compounds were synthesized with good yield and three of these presented (5a, 5l and 5p) good cytotoxicity against C6 cell line. Both affected cell cycle distribution via arresting more C6 cell line at Sub-G1 phase promoting apoptosis. Furthermore, 5a, 5l and 5p modulated redox status. These findings suggest that these compounds can be considered as promising lead molecules for further development of potential antitumor agents.

Potential Antitumor Agents X: Synthesis and Antitumor Activity of Two Nitrogen Mustard Derivatives Related to Ketocaine

1984 ◽  
Vol 73 (8) ◽  
pp. 1175-1177 ◽  
Author(s):  
Aldo Andreanix ◽  
Daniela Bonazzi ◽  
Mirella Rambaldi ◽  
Iraklis Galatulas ◽  
Rosaria Bossa
Keyword(s):  
Antitumor Activity ◽  
Nitrogen Mustard ◽  
Antitumor Agents ◽  
Potential Antitumor
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