Hatem S. Ali

Some pyrazole and pyrazolo[3,4-d]pyrimidine derivatives: synthesis and anticancer evaluation.

5‐Amino‐1‐p‐tolyl‐1H‐pyrazole‐4‐carbonitrile (1) was used for the preparation of some novel pyrazoles and pyrazolo[3,4‐d]pyrimidines 2–10. Moreover, the cytotoxicity and in vitro anticancer activities of the prepared compounds were also assessed against the MCF‐7 breast cancer, HepG2 liver cancer, and A549 lung carcinoma cell lines, along with investigation of the effect of the synthesized compounds on the expression of urokinase plasminogen activator (uPA). The tested compounds exhibited remarkable cytotoxic activity against MCF‐7 and HepG2 cells. Among the tested compounds, 2 and 9 revealed promising anticancer activity compared to the activity of the commonly used anticancer drug, doxorubicin, by inhibiting the expression of uPA.

Anticancer evaluation of some newly synthesized N-nicotinonitrile derivative

Some novel N-nicotinonitrile derivatives 3-14 have been synthesized starting with compound 1. The key step of this work is the coupling between compound 1 and activated sugars to afford the corresponding cyclic nucleosides 3-6. Moreover, the cytotoxicity and in vitro anticancer evaluation of the prepared compounds have also been assessed against breast MCF-7 cancer, liver HepG2 cancer and lung A549 carcinoma cell lines with investigation the effect of the synthesized compounds on the expression of urokinase plasminogen activator (uPA). The results revealed that, although all the compounds showed no anticancer activity against A549 cells without showing any effect on the expression of uPA, the tested compounds exhibited remarkable cytotoxicity activity against MCF-7 and HepG2 cell lines. Among the tested compounds, compounds 11 and 12 revealed promising anticancer activity compared to the activity of the commonly used anticancer drug, doxorubicin with inhibiting the expression of uPA.

New Pyrimidinone and Fused Pyrimidinone Derivatives as Potential Anticancer Chemotherapeutics

A series of novel substituted pyrimidinones and fused pyrimidinones (compounds 3–18) were synthesized starting with oxiranylmethanone 2. The in vitro cytotoxicity against a human breast adenocarcinoma (MCF‐7) cell line was investigated and most of the tested compounds showed potent cytotoxic activity against the MCF‐7 cell line comparable to the activity of the commonly used anticancer drug cisplatin. Treatment of MCF‐7 cells with increasing doses (2, 5, 10, and 20 µg/mL) of the tested compounds revealed that the activity of superoxide dismutase and the level of hydrogen peroxide were significantly increased, while the activities of catalase and glutathione peroxidase and the levels of reduced glutathione were significantly lowered compared with control MCF‐7 cells. In general, derivatives 11 and 16 revealed the highest anticancer activity among the tested compounds.

Taurine is absent from amino components in fruits of Opuntia ficus-indica

Juices of edible fruits from Opuntia ficus-indica (L.) Miller, commonly named prickly pears or Indian figs, were analysed for amino acids using an automated amino acid analyser run in the high-resolution physiological mode. Emphasis was put on the detection of free taurine (Tau), but Tau could be detected neither in different cultivars of prickly pears from Italy, South Africa and the Near East nor in commercially available prickly pear juices from the market.

Synthesis and Isomerization of Some Novel Pyrazolopyrimidine and Pyrazolotriazolopyrimidine Derivatives

4-Imino-1-p-tolyl-1,4-dihydropyrazolo[3,4-d]pyrimidin-5-ylamine (2) and (1-p-tolyl-1H-pyrazolo[3,4-d]pyrimidin-4-yl)-hydrazine (3) were prepared starting from ethyl 4-cyano-1-p-tolyl-1H-pyrazol-5-ylimidoformate (1). The structure of compound 3 was confirmed through preparation of the pyrazole derivatives 4 and 5. Also, the synthesis and structural characterization of pyrazolo[4,3-e][1,2,4]triazolo[4,3-c]pyrimidine derivatives 7 and 9 and their isomerization to pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine derivatives 6 and 8, respectively, under different suitable reaction conditions were reported. Moreover, the syntheses of 2-substituted-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine derivatives 10 and 11 was described.

Aroma volatile compounds of parsley cultivated in the Kingdom of Saudi Arabia and Egypt extracted by hydrodistillation and headspace solid-phase microextraction

ABSTRACT Thirty-nine volatile compounds identified in hydrodistilled essential oil (HD) of Egyptian parsley, representing 97.87% of the total oil, while solid-phase microextraction (HS-SPME) revealed 16 components constituting 96.54% of the volatile material. Monoterpenes were the predominant in both extracts with considerable quantitative differences, while a dramatic decrease in myristicin from 26.21% in HD extract to 4.87% in HS-SPME extract occurred. Myristicin, β-phellandrene and myrecene were the major components among 38 identified components accounting for 92.87% of the total identified volatiles in Madinah hydrodistillate. Parsley essential oil of Madinah exhibited a higher scavenging ability for 2,2ʹ-diphenyl-1-picrylhydrazyl in comparison to Egyptian parsley oil.