Synthesis and antitumor testing of certain new fused triazolopyrimidine and triazoloquinazoline derivatives

AbstractNew series of 1,2,4-triazolopyrimidine and 1,2,4-triazoloquinazoline derivatives were designed, synthesized, and evaluated for their antitumor activity. Compounds 6, 11, 26, 29, 41, 44, 48, 49 and 58 were tested as antitumor agents by the use of DNA-binding assay on TLC-plates, colorimetric assay for the degree of DNA-binding (Methyl green-DNA displacement assay), evaluation of antineoplastic activity against Ehrlich Ascites Carcinoma in mice, and finally modulation of apoptosis. 5-Flurouracil, vitamin C and ethidium bromide were used as positive controls in these techniques. Compound 26 proved to be the most active member of these series as antitumor agent with IC50 value of 47±1. Several characteristic features were observed to be essential for activity such as the morpholine group and the phenylazo group, in addition the electron-withdrawing groups favor the activity than the electron-donating ones

Synthesis and in vitro antioxidant activity of some new fused pyridine analogs.

A new series of pyrano[3,2-c]pyridines, pyrazolo[4,3-c]pyridines, and pyrido[4,3-d]pyrimidines were synthesized and screened for their in vitro antioxidant activity. Compounds 13, 14, 15, 23, 29, 30, and 31 exhibited the most active oxygen free-radical scavenger activity with percentage inhibitions of 99.4, 99.6, 99.8, 97.3, 99.0, 99.3, and 99.5%; respectively, which is comparable to the curcumin potency. Most of the tested compounds proved to be safe towards peripheral multinuclear neutrophils (PMNs). The detailed synthesis and antioxidant activity data are reported

4-[(1,3-Dioxoisoindolin-2-yl)methyl]benzenesulfonamide

The title compound, C15H12N2O4S, is V-shaped with the isoindoline ring system (r.m.s. deviation = 0.006 Å) inclined to the benzene ring by 84.27 (13)°. In the crystal, inversion dimers are formed via pairwise N—H...O hydrogen bonds. These dimers associate further into corrugated ribbons, via pairwise N—H...O and C—H...O hydrogen bonds, propagating along the a-axis direction and lying parallel to (001)

N-(12-Amino-9,10-dihydro-9,10-ethanoanthracen-11-yl)-4-methylbenzenesulfonamide

The title compound, C23H22N2O2S, crystallizes with the 4-methylbenzenesulfonamide entity oriented towards the center of the bridgehead C atoms with a C—N—S—C torsion angle of −61.3 (2)°. The molecule features an intramolecular N—H...N hydrogen bond. Weak C—H...O and C—H...π interactions aid in forming the three-dimensional supramolecular structure

N-(3-Aminobicyclo[2.2.1]heptan-2-yl)-4-methylbenzenesulfonamide

In the title compound, C14H20N2O2S, the sulfonamide O atoms lie to one side of the benzene ring and the aminobicycloheptanyl to the other side [Car—S—N—C torsion angle = −57.93 (11)°; ar = aromatic]. An intramolecular N—H...N hydrogen bond is formed. In the crystal, a supramolecular chain is formed along the b axis via N—H...O and N—H...N hydrogen bonds