We have recently identified a new class of compounds that selectively kill cells that express P-glycoprotein (P-gp, MDR1), the ATPase efflux pump that confers multidrug resistance on cancer cells. Several isatin-beta-thiosemicarbazones from our initial study have been validated and a range of analogues synthesized and tested. A number demonstrated improved MDR1-selective activity over the lead,...

The inhibition of corrosion of mild steel in hydrochloric acid by isatin glycine (ING) and isatin (IN) at 30-60 o C and concentrations of 0.0001 M to 0.0005 M was studied via weight loss method. At the highest inhibitor concentration studied ING exhibited inhibition efficiency of 87% while IN exhibited 84% at 60 o C. A chemical adsorption mechanism was proposed on the basis of the temperature e...

A number of N-arylmethyl substituted indole derivatives have been synthesized and their effectiveness against ADP and arachidonic acid induced platelet aggregation in human plasma was determined. The desired compounds were synthesized by reacting the appropriate aniline derivative with isatin (or substituted isatin) to form the corresponding imine structures. The so formed compound was then act...

Hydrazones and their derivatives constitute a versatile class of compounds in organic chemistry. The development of novel hydrazones containing compounds possess a wide verities of biological activities like as antioxidant, anti-inflammatory, anticonvulsants, antidepressant and anxiolytic, antihypertensive, anticancer, antimicrobial, anti-tuberculosis, and antifungal activity. Hydrazones posses...

the interaction between isatin-β-thiosemicarbazone (ibt) and calf thymus dna (ct-dna) was investigated in physiological buffer (ph 7.4) using neutral red (nr) dye as a spectral probe by uv–vis absorption and fluorescence spectroscopy, as well as viscosity measurements. the ibt is stabilized by intercalation in the dna ( k [ibt –dna] =1.03×105 m−1), and displaces the nr dye from the nr–dna comple...

Sorbent materials based on a hydrazone Schiff base compound, C(14)H(11)BrN(4)O(4), were prepared either by immobilizing the ligand into sol-gel (SG1) or bonding to silica (SG2). The sorbent materials were characterized by FT-IR, EDX, SEM, TEM, and TGA. The sorption characteristics of a matrix of eight transition metal ions (Ag(+), Cu(2+), Co(2+), Ni(2+), Fe(3+), Pb(2+), Zn(2+), and Mn(2+)) usin...

N-(4-tert-butylbenzoyl)-2-hydroxy-1-naphthaldehyde hydrazone (BBNH) inhibits both the DNA polymerase and ribonuclease H (RNase H) activities of the human immunodeficiency virus type 1 reverse transcriptase. In this study, we show that BBNH binding impacts on the stability of the human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) heterodimer. The Gibbs free energy of dimer di...

The title compound, [Ru(C10H8N2)2(C16H12N4O)](BF4)2·3CH2Cl2, crystallizes with one complex dication, two BF4 (-) counter-anions and three di-chloro-methane solvent mol-ecules in the asymmetric unit. The central Ru(II) atom adopts a distorted octa-hedral coordination sphere with two 2,2'-bi-pyridine (bpy) and one quinoline-2-carbaldehyde (pyridine-2-carbon-yl)hydrazone (HL) ligand. The hydrazone...

Introduction Methicillin-Resistant Staphylococcus aureus (MRSA) and Vancomycin-Resistant Enterococcus (VRE) have accomplished important rates of colonization and infection in most intensive care units. These multidrug-resistant strains of MRSA and VRE have been causing serious problems in health care. The rising clinical importance of drug-resistant pathogens has lent necessity to drug developm...