Resveratrol, a natural phytoalexin, exhibits a remarkable range of biological activities, such as anticancer, cardioprotective, neuroprotective and antioxidant properties. However, the therapeutic application of resveratrol was encumbered for its low bioavailability. Therefore, many researchers focused on designing and synthesizing the derivatives of resveratrol to enhance the bioavailability a...

[reaction: see text] The Silyl-Hilbert-Johnson reaction as well as the nucleobase-anion glycosylation of a series of 7-deazapurines has been investigated, and the 7-functionalized 7-deazapurine ribonucleosides were prepared. Glycosylation of the 7-halogenated 6-chloro-2-pivaloylamino-7-deazapurines 9b-d with 1-O-acetyl-2,3,5-tri-O-benzoyl-D-ribofuranose (5) gave the beta-D-nucleosides 11b-d (73...

2-Tosylacetonitrile (1) when reacted with α,β-unsaturated nitriles 2a-c or a mixture of formaldehyde and 3-amino-2-substituted-pent-2-endinitriles 6a,b yielded pyridine derivatives 3a-c and 9a,b, respectively, while when subjected to react with salicylaldehyde yielded chromene derivatives 4 and 5, subsequently. The behavior of thiocarbamoyl derivative 10 derived from 1 towards some α-halogenate...

There has recently been an increasing interest in controlling macromolecular conformations and interactions through halogen bonding. Halogen bonds are favorable electrostatic interactions between polarized, electropositive chlorine, bromine, or iodine atoms and electronegative atoms such as oxygen or nitrogen. These interactions have been likened to hydrogen bonds in terms of their favored acce...

Bisphenol-A (BPA) is one of the highest-volume chemicals produced worldwide and the widespread exposure of individuals to BPA is suspected to affect a variety of physiological functions, including reproduction, development, and metabolism. Its estrogenic activity has been well documented in the last 15 years. In addition to estrogen receptors, BPA has been also shown to bind to and activate the...

A new series of 3-substituted (methyl, ethyl or phenyl)-3H-quinazolin-4-one derivatives (4a-l) were synthesized through condensation reaction of their potassium salts (3a-l) with methyl, ethyl and phenylisocyanate. The newly synthesized derivatives (4a-l) were evaluated for anticonvulsant activity. It was found that these compounds showed the highest anticonvulsant activity at low doses (50-100...

Abstract The structures of the isomeric 2,5-dihydrothiophene 1,1-dioxide [orthorhombic, a = 11.340(2), b 7.0887(15), c 6.2811(13) Å, space group Pnma ] and 2,3-dihydrothiophene 6.3903(13), 7.2783(16), 11.075(2) have been determined show perfectly planar rings with expected bond lengths angles. In contrast, halogenated derivatives 3,3,4,4-tetrachlorotetrahydrothiophene [monoclinic, 11.8716(8), 6...

Enzymes AKR1C regulate the action of oestrogens, androgens, and progesterone at pre-receptor level are also associated with chemo-resistance. The activities these oestrone halides were investigated on recombinant enzymes. halogen atoms both C-2 C-4 positions (13?-, 13?-methyl-17-keto derivatives) most potent inhibitors AKR1C1. lowest IC50 values for 13?-epimers 2_2I,4Br 2_2I,4Cl (IC50, 0.7 ?M, ...