We describe sequence-specific alkylation in the minor groove of double-stranded DNA by a hybridization-triggered reactive group conjugated to a triplex forming oligodeoxyribonucleotide (TFO) that binds in the major groove. The 24 nt TFOs (G/A motif) were designed to form triplexes with a homopurine tract within a 65 bp target duplex. They were conjugated to an N 5-methyl-cyclopropapyrroloindole...

J . R a d h a k r i s h n a n Department of Chemistry, University of Connecticut, Storrs, Connecticut 06268, USA Z. Naturforsch. 84b, 481-487 (1979); received August 15, 1978 Solvolysis, Methylnorbornyl Systems, Norbornan-3,6-dione, 2-exo-Methylnorbornan-6-one 3-Nortricyclyl bromide (11) was transformed in four steps to norbornan-3,6-dione (10). Methyl 4 -hydroxy-2-butynoate (19) was prepared f...

Direct C2-alkylation of an indole bearing a readily removable N-pyrimidyl group with a vinylsilane was achieved by using a cobalt catalyst generated in situ from CoBr(2), bathocuproine, and cyclohexylmagnesium bromide. The reaction allows coupling between a series of N-pyrimidylindoles and vinylsilanes at a mild reaction temperature of 60 °C, affording the corresponding alkylated indoles in mod...

N-Demethylvancomycin, which has been clinically used in China, is one member of vancomycin group (glycopeptide) antibiotics. It differs from vancomycin only in that methyl group on the amino group of the N-terminal residue of vancomycin has been replaced by H. By reductive alkylation of N-demethylvancomycin, we synthesized N-alkyl and N,N'-dialkyl N-demethylvancomycins, which closely correlated...

Male Sprague-Dawley (Charles River CD) rats received a single carcinogenic dose (12 mg/kg) of the a-acetoxy deniva tive of dimethylnitrosammne,N-[14C]methyl-N-acetoxymethylni trosamine, and were allowed to survive for 12 hr. Following iv. injection, highest Concentrations of 7-methylguanine and Q6@ methylguanine were present in DNA of the lung, the principal target organ in the carcinogenesis b...

Doubly protonated substance P and two analogs alkylated at the ninth position was studied to determine the effect of N-alkylation of the amide nitrogen on the electrospray ionization/surface-induced dissociation (ESI/SID) fragmentation pattern. Thermal decomposition experiments and ab initio calculations were also used in conjunction with the ESI/SID experiments. The increase in relative abunda...

We report herein a feasible study concerning syntheses and structure of some diazolium salts with dihydroxyacetophenone skeleton of anticipated anticancer activity. A fast, general and facile method for preparation of 1,3-diazol salts via N-alkylation reactions under conventional heating and microwave irradiation is presented. The microwaves remarkably accelerated these N-alkylations, the react...

The alkylation of purines which is generally carried out after anion formation by treatment with a base and alkyl halide complicated in the best cases, mixtures N-alkylated compounds are obtained. Purine derivatives can be acquired from at N-7 N-9. In this work, reaction conditions have been optimized to obtain products N-9 regioselectively. Different bases tried tetrabutylammonium hydroxide ha...