The synthesis of several halogenated benzimidazoles substituted in position 2 with trifluoromethyl, pentafluoroethyl and 2-thioethylaminodimethyl group is reported. Antiprotozoal and anticancer activity of series of newly synthesized and previously obtained compounds was studied. All of tested b...

The aim of the present study was to examine the inhibitory effects in vitro of the affinity ligands 14-β-chloroacetylnaltrexone (CAN) and 14-β-bromoacetamidomorphine (BAM) to characterize the pharmacological specificity of the ligands for high and low affinity opioid binding sites. Rat brain m...

Sodium acetate catalyzed assembling of salicylaldehydes, malononitrile and 4-hydroxy-6-methylpyridin-2(1H)-one in small amount of ethanol gives rapidly (5 min) substituted 4-pyridinyl-2-amino-4H-chromenes in 82–99% yields. This novel domino reaction opens the fast, facile, and flexible way to t...

Cigarette smoke can cause follicle destruction and oocyte dysfunction and increase the risks of spontaneous abortion, stillbirth, and tubal ectopic pregnancy, affecting female reproductive health. Third-hand smoke (THS) is residual tobacco smoke existing in the environment long after cigarettes ...

A new method for preparing optically active 1,3-dioxin-4-one derivatives is presented. A series of prochiral 2,2-bis(hydroxymethyl)-1,3-dioxin-4-ones was synthesized by [4+2]cycloaddition of acylketene to protected 1,3-dihydroxy-2-propanone derivatives followed by deprotection of the hydroxyl gr...

A series of 2-aryloxycarbonylthiophene-3-sulfonamides were synthesized and evaluated to determine their antagonistic activity at the endothelin receptors. N-(4-chloro-3-methyl-5-isoxazolyl)-2-[(3,4-methylenedioxy)phenoxycarbonyl]thiophene-3-sulfonamide was identified as a highly selective, poten...

Two series of 2-aminopyridine derivatives 6-17 and tyrphostin AG17 analogs 18-22 bearing 4-methylbenzenesulfonamide moiety were designed and synthesized as anticancer compounds. The synthesized compounds were biologically evaluated for their cytotoxic activity against human breast cancer cell li...

Corticotropin releasing factor (CRF) is a neuropeptide hormone produced from the hypothalamus that controls the secretion of corticotropin (ACTH) from the anterior pituitary gland that, in turn, prompts the adrenal glands to secrete glucocorticoids. This involvement in the hypothalamic–pituitar...

Acyclic nucleoside 2-amino-6-(4-methoxyphenylthio)-9-[2-(phosphonomethoxy)ethyl]purine bis(2,2,2-trifluoroethyl) ester (ABE, 1) is a new hepatitis B virus (HBV) specific antiviral reagent and shows high anti-HBV activity. Carbon-11 labeled ABE may serve as a novel reporter probe for positron emi...

A number of new diazabenzo[e]acephenanthrylene-1,2-dicarboxylate derivatives have been prepared regiospecifically in moderate to good yields from the triphenylphosphine-mediated cyclocondensation reaction of dialkyl acetylenedicarboxylates with 1-(4-aryl)-2-(11H-indeno[1,2-b]quinoxalin-11-yliden...

A series of pyridine and thieno[2,3-b]pyridine derivatives have been designed and synthesized as anticancer PIM-1 kinase inhibitors. Thirty-seven compounds were selected by NCI to be tested initially at a single dose (10 µM) in the full NCI 60 cell line panel. Compound 5b showed potent anticanc...

S-Benzyl-β-N-[3-(4-hydroxy-3-methoxy-phenylallylidene)]dithiocarbazate (HL1), Schiff base of S-benzyl dithiocarbazate, was synthesized by 1:1 condensation between S-benzyl dithiocarbazate and 4-hydroxy-3-methoxy cinnamaldehyde. The nitrogen-sulfur Schiff base (HL1) was characterized by Mass, FT...

A series of (1-aryl-1H-pyrazol-4-yl) (3,4,5-trimethoxyphenyl)methanones (8a-p, 9a-p) and ketoxime (10c) derivatives were designed and synthesized as antitubulin agents. All of the target compounds were evaluated for the in vitro anti-proliferative activities against three tumor cell lines (A549,...

Existing antifolate antimalarial drugs have shown resistance due to the mutations at some amino acid positions of Plasmodium falciparum DHFR-TS. In the present study, to overcome this resistance, a new series of hybrid 4-aminoquinoline-triazine derivatives were designed and docked into the activ...

The stereochemistry of syn and anti-forms of bridged bicyclo[3.n.1]-2-ene, tricyclo[7.n.1.0]-2-ene (n=1–3) and bicyclo[4.3.1]dec-7-ene derivatives can be assigned from the 13C chemical shift difference of the double bond. Both syn-9-R-bicyclo[3.3.1]non-2-enes and syn-13-R-tricyclo[7.3.1.02,7]tr...

Chlorinated 2-phenoxyphenols containing 3 to 7 chlorine atoms were synthesized and their structures determined by NMR and GC-MS. The most characteristic MS properties and GC retention times of the free phenols and their ethyl derivatives were investigated. The results were applied to analysis of...

The photochemical and thermochemical decompositions of a trichloro- and a pentachloro-2-phenoxyphenol have been studied. The photolysis of the pentachloro-2-phenoxyphenol, which is one of the impurities found in commercial 2,4,6-trichlorophenol, gave 1,2,3,8-tetrachlorodioxin, two trichlorodioxi...

Polystyrene supported N-phenylpiperazine-Pd(II) complex D was synthesized and characterized by various techniques, including Fourier transform infrared spectroscopy (FTIR), scanning electronmicroscopy (SEM), energy dispersive X-ray spectroscopy (EDX) and thermal analysis (TG-DTA). This heterogen...

Copper(II), zinc(II) and platinum(II) complexes of phenylpiperazine dithiocarbamate formulated as [CuL2], [PtL2] and [Zn2(μ-L)2(L)2], where L = phenylpiperazine dithiocarbamate were prepared and characterized by elemental analysis IR, UV–Visible, 1H and 13C NMR spectroscopy. Single crystal X-r...

Described in this report is a systematic study which led to the identification of two new dopamine D2 partial agonists (5 and 17). Phenols 5 and 17 represent prototypes of two new classes of D2 partial agonists as well as templates for the future design of novel dopaminergic agents.