scholarly journals Utility of Activated Nitriles in the Synthesis of Novel Heterocyclic Compounds with Antitumor Activity

2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
Asmaa S. Salman

Reaction of cyanoacetic acid hydrazide (1) with 4-methoxyacetophenone and 4-chlorobenzaldehyde (2a,b) afforded the corresponding 2-cyanoacetohydrazide derivatives (3a,b) respectively. The latter compounds were utilized as a key intermediate for the synthesis of new heterocyclic compounds. Newly synthesized compounds were characterized by elemental analyses and spectral data. The antitumor evaluation of some newly synthesized compounds was screened in vitro against human breast cancer cell line (MCF-7).

Author(s):  
Ana Catarina Viana Valle ◽  
Lana Ribeiro Aguiar ◽  
Hilana dos Santos Sena Brunel ◽  
Patricia Furtado Malard ◽  
Carla Lujan Pereira Villarroel ◽  
...  

BACKGROUND Adenocarcinomas can be of several types, and MCF-7 is an adenocarcinoma of human breast cell line useful as preclinical model to screen therapeutic agents such as ultra-diluted Viscum album, an European plant whose extract is commonly used in cancer therapy. AIMS MCF-7 and mesenchymal stem cells were used to evaluate the in vitro cytotoxicity of homoeopathic Viscum album 1x10-3 (VAD3). METHODS cells were cultured for 24 hours in controlled environment (37.5oC and 5% CO2) in 96-well plates. After this time, VAD3 was added to the culture medium in concentrations varying from 10 to 100 ?L/mL for MTT assay (evaluation of viability of cells). A control group was maintained with culture medium only. After 48 hours, the procedures of analysis of cells viability were performed. RESULTS MTT assay showed that the concentrations of 42 ?L/mL and 62 ?L/mL were able to reduce cell viability to 50% in MCF-7 and mesenchymal stem cells, respectively, which means that half of the cells cultured were dead after 48 hours in contact with VAD3. CONCLUSION Viscum album presented higher cytotoxic action on human breast cancer cell line culture than on mesenchymal stem cells. This medicine is extensively used against cancer, and the use of the homoeopathic form of it brings new possibilities as no or fewer adverse effects would be present.


2011 ◽  
Vol 26 (1) ◽  
pp. 105-111 ◽  
Author(s):  
Ayfer Yurt Kilcar ◽  
F. Zumrut Biber Muftuler ◽  
Perihan Unak ◽  
Cigir Biray Avci ◽  
Cumhur Gunduz

Breast Cancer ◽  
1999 ◽  
Vol 6 (2) ◽  
pp. 87-92 ◽  
Author(s):  
Akihiko Suto ◽  
Nitin T. Telang ◽  
Hirokazu Tanino ◽  
Toshio Takeshita ◽  
Harumi Ohmiya ◽  
...  

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (12) ◽  
pp. 28-31
Author(s):  
D Nikam ◽  
◽  
S. Tanvar ◽  
A Kute ◽  
S Lokhande ◽  
...  

A series of dihydropyrimidone derivatives was synthesized by an efficient, simple and solvent less green method by using Beginelli reaction. Various aromatic aldehydes, urea and ethyl acetoacetate were refluxed for a few hours and the reaction monitored by periodic TLC (hexane: ethyl acetate 6:4 v/v) and products are purified by recrystallization, with characterization by FTIR, 1H NMR. All the purified compounds were subjected to evaluatation by in vitro human breast cancer cell line MDA-MB-231 and MCF-7. Compound I-k was found to be moderately active against MCF-7 with GI 50 value of -4.38.


2017 ◽  
Vol 13 (2) ◽  
pp. 5959-5976
Author(s):  
Alaa M. Hayallah

An olomoucine analogues of 2-[(1-substituted)-2,6-dioxo-2,3,6,7–tetrahydro-1H-purin-8-ylsulfanyl]-N-substituted acetamide 6a-g and 7a-g, 1-substituted-8-[2-(4-substituted phenyl)-2-oxoethylsulphanyl]-3,7-dihydro-1H-purine-2,6-diones 9a-g and 10a-g, 3-(2-substituted benzyl)-6-(4-substituted phenyl)-1H-thiazolo[2,3-f]purine-2,4-dione 11a-g and 12a-g and their isosteres 3-substituted benzyl-5-methyl-7-substituted-1H-pyrido[2,3-d]pyrimidine-2,4-dione 13a-c and 14a-c were designed and synthesized. The target compounds 11a-g and 12a-g were prepared by cyclodehydration of 9a-g and 10a-g in PPA, while 13a-c and 14a-c were synthesized by condensation of 6-amino-3-(2-substituted benzyl)-1H-pyrimidine-2,4-dione 1a or 1b and the appropriate acylacetone in glacial acetic acid. Structures of the new compounds were verified on the basis of their IR, 1H NMR, MS, HRMS and elemental analyses. The newly synthesized compounds were tested for their anticancer activity and most of the tested compounds showed good to excellent inhibition activity against the tested human breast cancer cell line MCF-7 in comparison to doxorubicin as a reference drug. KEYWORDS: olomoucine; cyclin-depenent kinase; synthesis; anticancer  


2019 ◽  
Vol 97 (1) ◽  
pp. 53-60 ◽  
Author(s):  
Sherif M.H. Sanad ◽  
Azza M. Abdel-Fattah ◽  
Fawzy A. Attaby ◽  
Mohamed A.A. Elneairy

The novel 1,4-bis(2,6-dibromo-4-formylphenoxy)butane (3), prepared from 3,5-dibromobenzaldehyde (1), reacted with different hydrazines 4a–4d and active methylene containing compounds 9a–9d to give the corresponding bis(hydrazones) 5a–5d and bis(cinnamonitriles) 11a–11d, respectively. Both bis(2-cyanoacetic acid hydrazide) derivative 5d and bis(thioacrylamide) derivative 11a were taken as synthetic precursors for the synthesis of the target molecules bis(pyridine-2(1H)-thione) derivative 10 and 13a–13c and their bis(2-methylsulfanylpyridine) derivative 14 and 17a–17c. Another synthetic route was designed to prepare the target molecules 14 and 17a–17c in a better yield using pyridine-2(1H)-thione) derivative 15 and 19a–19c. Characterization of the newly prepared compounds via elemental analyses and spectral data are established.


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