The metabolism of 7-methylbenz(a)anthracene by rat-liver preparations and by mouse skin has been studied using a combination of thin-layer and high pressure liquid chromatography and all five possible trans-dihydrodiols have been detected as metabolites but in different proportions. The roles of...

The metabolism of 7-ethyl (7-EBA) and 7-methylbenz[a]anthracene (7-MBA) to dihydrodiols has been compared in incubations with hepatic microsomal fractions prepared from untreated rats. Although both hydrocarbons were found to be metabolised to similar extents, the relative proportions of their d...

Benz[a]anthracene (BA) and its derivatives containing methyl and/or ethyl groups in the 7 and/or 12 positions were tested for their ability to induce chromosome aberrations (CA) in rat bone marrow cells and for their mutagenicity to Salmonella typhimurium TA100 or TA98. The incidence of aberrant...

Benz[a]anthracene (BA) and the monomethyl meso-anthracenic or L-region derivatives 7-methylbenz[a]anthracene (7-methylBA) and 12-methylbenz[a]anthracene (12-methylBA) underwent a bioalkylation substitution reaction in rat lung ctyosol preparations, fortified with S-adenosyl-l-methionine to form ...

The carcinogenicity of a number of ethylated analogs of 7,12-dimethylbenz[a]anthracene (DMBA) has been previously studied. The covalent binding of these compounds to mouse embryo fibroblast 10T12 cell DNA expressed as adducts/106 bases, paralleled the original carcinogenicity studies and in decr...

Photolysis of 9-methyl-10-nitroanthracene in chloroform or methanol produces mainly two products 9-methyl-9-nitrosoanthracen-10-one and 9,10-anthraquinone in about 4:1 ratio under ambient air. The formation of 9-methyl-9-nitrosoanthracen-10-one confirms the proposed excited state rearrangement r...

The Suzuki reaction has been applied to provide a highly abbreviated synthesis of 5-methylchrysene and its 2-hydroxy- and 8-hydroxy derivatives from easily accessible starting materials.

Stereospecific syntheses of the trans-3,4-dihydrodiol metabolites of 9- and 10-fluoro-7,12-dimethylbenz[a]anthracene, -7-methylbenz[a]anthracene, and -12-methylbenz[a]anthracene are described. These dihydrodiols are putative proximate carcinogenic metabolites that undergo activation by the P-450...

A series of compounds consisting of 2-alkoxy, 2-acyl, and 2-hydroxy-5-alkyl-5-nitro-1,3,2-dioxaphosphorinane 2-oxides has been prepared. Several amine salts of the 2-hydroxy compounds have been isolated. All of the compounds prepared were submitted for antitumor evaluation.

Twenty-two of the title compounds, in which the substituents are chloro, alkylamino, dialkylamino, arylamino, hydroxy, and amine salts, as well as the pyrophosphate, have been synthesized and submitted for antitumor evaluation.

A series of 2-substituted-5-alkyl-5-nitro-1,3,2-dioxaphosphorinane 2-oxides consisting of 2-alkylamino and 2-arylamino types have been prepared and submitted for antitumor screening.

A phosphorus-containing flame retardant, 5,5-dimethyl-1,3,2-dioxaphosphorinane-2-(2,4,6-tribromophenoxy)-2-oxide(DPDMO), was synthesized successfully and characterized by elemental analysis (EA), mass spectra (MS), infrared spectroscopy (FT-IR) and nuclear magnetic resonance (1H NMR and 13C NMR)...

A biotechnological approach was adopted for increasing foliar ascorbate levels as a strategy to adapt a widely grown high yielding rice variety to multiple abiotic stresses. The variety IR64 (Oryza sativa L. ssp. indica) was engineered to express the ascorbate biosynthesis gene GDP-L-galactose p...

Reactions of Co(II) acetate with 1-benzoyl-(3-methyl-3-R)thiourea (R = ethyl, propyl, cyclohexyl and phenyl) and 1-benzoyl-(3-ethyl-3-benzyl)thiourea ligands, herein refer to as 1-benzoyl-(3,3-disubstituted)thiourea, derived from secondary alkyl- and arylamines gave [tris(1-benzoyl-(3,3-disubsti...

Six new Co(II) and Co(III) complexes (1–6) of di-2-pyridyl ketone N(4)-cyclohexyl thiosemicarbazone (HL1) and di-2-pyridyl ketoneN(4)-phenyl thiosemicarbazone (HL2) have been synthesized and spectrochemically characterized. HL1 is newly synthesized and has been structurally characterized by sin...

A series of 2-[2-(substituted benzylidene) hydrazinyl]-4-(4-methoxyphenyl)-6-oxo-1,6-dihydro-pyrimidine-5-carbonitrile (3–16) were synthesized by refluxing 2-hydrazino-4-(4-methoxy-phenyl)-6-oxo-1,6-dihydro-pyrimidine-5-carbonitrile (2) with different substituted aromatic aldehydes in glacial a...

In the present study, a new class of compounds containing pyrido[3,4-d]pyrimidine scaffold with an acrylamide moiety was designed as irreversible EGFR-TKIs to overcome acquired EGFR-T790M resistance. The most promising compound 25h inhibited HCC827 and H1975 cells growth with the IC50 values of ...

A new class of corticotropin releasing factor 1 (CRF1) receptor antagonists characterized by a tricyclic core ring was designed and synthesized. Novel tricyclic derivatives 2a–e were designed as CRF1 receptor antagonists based on conformation analysis of our original 2-anilinobenzimidazole CRF1...

A series of novel 7-indole substituted 2,4-diamino-5,8-dihydropyrido[2,3-d]pyrimidine analogous to the 2,4-diaminopteridine core were synthesized by the three-component one-pot cyclocondensation between 2,4,6-triaminopyrimidine, 3-(2-cyanoacetyl)indole and aromatic aldehydes. The reactions, whic...

A series of new quinazolinone based mono azo reactive dyes (D1–10) have been prepared by subsequent diazotization of 2-phenyl-3-[4′-(4″-aminophenylsulphonamido)]phenyl-4(3H)-quinazolinone-6-sulphonic acid (C) and coupling with various 4-chloro anilino cyanurated coupling components. These dye...