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Synthesis and Biological Activity of Some New ..

Pyrimidines and their derivatives have been found to possess a broad spectrum of biological activities such as antimicrobial, anti-inflammatory, analgesic, antiviral and anticancer activities 2-9. The synthesis of furan derivatives has engrossed substantial attention from organic and medicinal chemists for many years as they belong to a class of compounds with proven utility in medicinal chemistry 10. Furan derivatives are known to be associated with multiple biological activities 11, 12. Therefore, both the pyrimidine and furan possess worthy and imperative bioactivities, which render them useful substances in drug research.

In view of these observations and in continuation of our research program on the synthesis of chalcones and their derivatives 13, 14, like pyrimidines, pyrazolines and isoxazolines, we report here in the synthesis of some new pyrimidine derivatives which have been found to possess an interesting profile of anticancer activity.

El-Kashef,, Synthesis and biological activity of some new pyrimidothienoquinoline,, Bull.

Synthesis of some new Benzofuro[3,2-d]pyrimidines of biological ..

Farghaly,, Synthesis, Reactions and Antimicrobial Activity of Some New Indolyl-1,3,4-Oxadiazole, Triazole and Pyrazole Derivatives.

Structure-based design, synthesis and biological evaluation of new small molecules anti-cancer agents were described. On continuation of applying scaffold hopping theory, a series of 5-arylthieno[2,3-]pyrimidines based on the structural features of lapatinib was designed, synthesized and characterized using IR, 1H-NMR, 13C-NMR, mass and microanalyses. Biological evaluation of the cytotoxic activity against MCF-7 cell line and the inhibition of the enzymatic activity of epidermal growth factor tyrosine kinase were carried out for the target compounds. Substituting the 4-anilino-5-arylthieno[2,3-]pyrimidines with different pharmacophoric groups at , and/or positions led to discovery of two potent lead compounds 3b and f with excellent cytotoxic activity and enzymatic inhibition activity.

Structure-based design, synthesis and biological evaluation of new small molecules anti-cancer agents were described. On continuation of applying scaffold hopping theory, a series of 5-arylthieno[2,3-]pyrimidines based on the structural features of lapatinib was designed, synthesized and characterized using IR, 1H-NMR, 13C-NMR, mass and microanalyses. Biological evaluation of the cytotoxic activity against MCF-7 cell line and the inhibition of the enzymatic activity of epidermal growth factor tyrosine kinase were carried out for the target compounds. Substituting the 4-anilino-5-arylthieno[2,3-]pyrimidines with different pharmacophoric groups at , and/or positions led to discovery of two potent lead compounds 3b and f with excellent cytotoxic activity and enzymatic inhibition activity.

Synthesis and Antidepressant Activity of Some New …

seven new pyrimidines were synthesized by following the standard procedures using substituted aromatic aldehydes, methyl ketones and metformin. After the biological activity was predicted using PASS, Molinspiration and Osiris property explorer, their anthelmintic activity was evaluated using Pheretima posthuma. The structural assignment of the title compounds (P1-7) has been made on the basis of elemental analysis, infrared, 1H-nuclear magnetic resonance and Mass spectral studies.

»Synthesis and antimicrobial activity of some new 1,3-thiazoles, ..

A number of 2-amino-4-(2', 5'-dimethyl-3'-furyl)-6-(aryl)-pyrimidines 4(a-n) have been synthesized by treating the 1-(2', 5'-dimethyl-3'-furyl)-3-(aryl)-2-propen-1-one (3a-n) with guanidine hydrochloride in presence of potassium hydroxide and ethanol. All these compounds were characterized by means of their IR, 1H NMR spectroscopic data and microanalyses. When these compounds were evaluated for anticancer activity, some of them were found to possess significant activity.

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Synthesis and Antidepressant Activity of Some New ..


Synthesis and Biological Activity of Some New …

RESULTS AND DISCUSSION: The title compounds 2-amino-4-(2', 5'-dimethyl-3'-furyl)-6-(aryl) pyrimidines (4a-n) were synthesized in good yields (scheme-I). Some of the compounds have significant anticancer activity against the cell lines (DU-145). Out of all the compounds, 4b containing 4-chlorophenyl substitution on 6th position of pyrimidine nucleus showed maximum activity, closely followed by 4e containing thiophene ring. These compounds also need to be tested on other cancer cell lines in order to predict their activity and therapeutic usefulness.

Biochemistry of Plasmodium --Brief Overview

As pyrimidine is a basic nucleus in DNA and RNA, it has been found to be associated with diverse biological activities. Pyrimidine derivatives were reported to possess anticonvulsant, antimicrobial, anti-inflammatory, antitumor, and antihistaminic. Recently, our team reported the anti-inflammatory and antimicrobial evaluation of some pyrimidines.

Biochemistry of Plasmodium--Brief Overview

El-Kashef., Synthesis, reactions and antimicrobial activity of some new 1,3,4-oxadiazoles, 1,2,4-triazoles and 1,3,4-thiadiazines derived from pyrazole,, Heterocyclic Communications, Vol.

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