Novel 1,2,4-oxadiazoles and trifluoromethylpyridines related to natural products: synthesis, structural analysis and investigation of their antitumor activity

Synthesis and in vitro antiproliferative activities of (5-aryl-1,2,4-oxadiazole-3-yl) methyl d-ribofuranosides

“…9 Pyrazole-pyrimidine derivatives bearing 1,2,4-oxadiazole were tested in vitro for anti-tumor activity in a panel of 12 human tumor cell lines, finding that N 3 -(4-(3-(tertbutyl)-1,2,4-oxadiazol-5-yl)phenyl)-6-phenyl-1H-pyrazolo[3,4d]pyrimidine-3,4-diamine has a moderate overall potency, combined with good selectivity towards the renal cancer cell line RXF 393. 10 4-Chloro-benzamides derivatives containing the 1,2,4-oxadiazole core, afforded a new class of receptor tyrosine kinase inhibitors, showing comparable activity to the multitargeted tyrosine-kinase inhibitor Ponatinib. 11 Considering that the 1,2,4-oxadiazolic ring is an important part of many biologically active compounds and the potential antitumor activity of the diheterocyclic 2,3-O-cyclopentylideneβ-D-ribofuranoside compounds, we envisioned the preparation of a small and focused library of compounds bearing both structural features.…”

“…Next, compounds 10a-d were converted to their corresponding tosyl The diheterocyclic compounds 13-14 were evaluated for their in vitro antiproliferative activity against the human cancer cell lines A549 (lung), HeLa (cervical), HBL-100 (breast), SW1573 (lung), T-47D (breast), and WiDr (colon). 14 In addition, compounds 2-4 and selected intermediates (10)(11)(12) were tested for comparison purposes. The results, expressed as GI 50 values, are shown in Table 1.…”

New strategy of synthesis, characterization, theoretical study and inhibition effect on mild steel corrosion in acidic solution

“…Considerable attention has directed toward finding heterocyclic organic compounds previously used in synthetic organic chemistry in many chemical areas. Heterocyclic systems have recently attracted much attention because they have various abilities such as anti-microbial, anti-tumor, anti-epileptic, antihistaminic, anti-oxidant and anti-inflammatory actions [1][2][3][4][5][6][7][8][9][10][11][12][13][14][15][16][17] ; and they are being used as lead compounds for drug development 18 . As the results of several recent studies have indicated that some heterocyclic compounds derivatives synthesized have a diversity of useful biological effects including antibacterial, antifungal, analgesic, antiviral, anticancer, antihypertensive, anticonvulsant, and anti-diabetic properties [19][20][21][22][23][24][25] .…”

A Theoretical Study of the Molecular Coupled Structures of Aristolochic Acids and Humic Acid, Potential Environmental Contaminants

“…The Aristolochia clematitis plant, which grows especially in areas of Romania, Bulgaria, Serbia, Bosnia, and Herzegovina, is considered as one of the Balkan endemic nephropathy cofactors; the first scientist who presented this hypothesis was Ivic . Other interesting plants (as Helleborus ), growing in this area, especially in Romania, or other heterocyclic derivatives, aromatic amines and heterocyclic phosphorous compounds, identified in other plants have interesting biological effects . There are recent studies regarding the uptake and accumulation of AAs by cucumbers and maize or by lettuce, tomato and spring onion cultivated in AA‐contaminated soil .…”