The overexpression of P-glycoprotein plays an important role in the process of multidrug resistance (MDR). P-gp inhibitors are one of the effective strategies to reverse tumor MDR. Novel P-gp inhibitors with phthalazinone scaffolds were designed, synthesized and evaluated. Compound 26 was found ...

Vitamin A ester degradation was studied in isopropyl alcohol, isopropyl alcohol and water, cyclohexane, and in these solvents containing members of the acetic acid series of fatty acids. The results indicate that (a) the principal methods of degradation are oxidation and elimination in hydroxyla...

Vitamin A esters of fatty acids having electronegative groups in the number 2 position were prepared. Acids, with chlorine or a double bond, were used and the esters were tested for stability against acid and solvolytic action. The results indicate that (a) stability against proton attack, in an...

Publisher SummaryThis chapter discusses the use of trichloroacetic acid method for colorific estimation of vitamin A in serum and liver tissue. In this method, trichloroacetic acid crystals (50 g), freshly washed with solvent, are dissolved in alcohol-free distilled chloroform (25 ml). This give...

Photo-oxidation of vitamin A with UV light gave retinal and a mixture of epoxy derivatives of the vitamin; however, vitamin A palmitate gave anhydrovitamin A and fragments derived from cleavage of the side-chain double bonds. The rate of oxidation and the type of oxidation products produced by p...

Of the several pathways by which vitamin A and its derivatives can degrade, the present study is concerned with those leading to the formation of anhydrovitamin A. Results indicate (a) anhydro formation does not occur readily with vitamin A alcohol in the absence of a strong catalyst such as hyd...

When anhydrovitamin A was fed to vitamin A-deficient rats, it was absorbed as such and converted over the next 48 h to hydroxylated derivatives and their esters. Large doses of anhydrovitamin A, if given every day, showed biological in the vaginal smear assay, promoted growth, and lowered the li...

Anhydrovitamin A was fed to vitamin A-deficient rats and its metabolites isolated from the livers. These consisted of two monohydroxy and one dihydroxy derivatives and their esters. None was identical with retro-vitamin A prepared chemically from vitamin A. Neither anhydrovitamin A nor its deriv...

The Raman spectrum of all-trans anhydrovitamin A in hexane at 77 degrees K is presented. The similarity of the Raman spectra of anhydrovitamin A and the protonated Schiff base of retinal is striking. The implications of this for visual pigment studies and bacteriorhodopsin are discussed. Tentati...

In view of the limited information available on functional significance of TRPV1 in regulating sperm functions, present study was undertaken on bull spermatozoa. Sixty four ejaculates were collected from four Hariana bulls and were used for molecular and functional characterisation of TRPV1. Imm...

A series of imidazo[4,5-c]pyridine-7-carboxamide derivatives as poly(ADP-ribose) polymerase (PARP) inhibitors have been developed. All target compounds were evaluated for their PARP-1 inhibitory activity and some were further assessed for cellular potency. These efforts led to identification of ...

The reaction of 2-oxo-N-arylpropanehydrazonoyl chlorides 3a–e with 3-methyl-2-benzofurancarboxylic acid hydrazide (7) furnished N-(aryl)propanehydrazonoyl chlorides 8a–e. X-Ray of 8c revealed the (1Z,2E) configuration of structure 8. Nucleophilic substitution reaction of 8a or 8d with piperidi...

The synthesis and in vitro anticancer activity of novel β-carbolines is reported. New tryptamines have been prepared via hetero-Diels-Alder reaction of nitrosoalkenes with indoles and used to prepare functionalized β-carbolines by the Pictet-Spengler approach. These included 6-substituted-β-c...

A total of 14 of 1,5-disubstituted tetrazole derivatives were prepared by reacting appropriate thiourea and sodium azide in the presence of mercury (II) chloride and triethylamine. All compounds were evaluated in vitro for their antimicrobial activity. Derivatives 10 and 11 showed the highest in...

The reactions of CuCl and CuBr with 2-amino-5-chloropyrimidine (L-Cl), 2-amino-5-bromopyrimidine (L-Br) and 2-amino-5-iodopyrimidine (L-I) in aqueous solutions of HCl and HBr afforded [CuCl2(HL-I) · H2O]n, 1, [CuBr2(HL-I) · H2O]n, 2, [CuCl2(HL-Br) · H2O]n, 3, [CuBr2(HL-Br) · H2O]n, 4, and [C...

A series of Ag(I) complexes containing the 2-amino-5-halopyrimidine ligands have been synthesized and their structures characterized by X-ray crystallography. The isomorphous complexes Ag(L-Cl)2(CF3SO3) (L-Cl = 2-amino-5-chloropyrimidine), 1, and Ag(L-Br)2(CF3SO3) (L-Br = 2-amino-5-bromopyrimidi...

The title cyclopentenone has been prepared by enzymatic resolution of cis-4-phenyloxy- and cis-4-(4-methoxyphenyloxy)-cyclopent-2-en-1-ol in isopropenyl acetate using Pseudomonas cepacia lipase. The use of a 4-methoxyphenyloxy-alcohol intermediate enabled the use of both enzymatically resolved e...

The treatment of hexahydro-1.3-pentalenedimethanol 1 with MCPB acid gave a pentalenofurane compound 7 instead of an epoxide, in >90% yield by participation of the closer hydroxymethyl group in epoxidation. Acyl-protected derivatives 1a–1e gave a mixture of exo- and endo-epoxides 5/6 as expected...

Thin films of zinc sulfide were prepared by ultrasonically spraying a toluene solution of bis(diethyldithiocarbamato)zinc(II) onto silicon, sapphire and gallium arsenide substrates at 460–520 °C. The films prepared on silicon or sapphire were found to have a highly oriented hexagonal structure...

Determination of the crystal structure of bis(diethyldithiocarbamato)dibromopalladium(IV) (I), shows it to have a distorted octahedral geometry, with the bromide ligands mutually cis. We also report the structure of a new palladium(II) complex, obtained as a decomposition product in the crystall...