Exposure of sarcoma 180 ascites cells to 2-amino-6-chloropurine (6-C1G) in vivo resulted in several metabolic lesions in the pathways of purine nucleotide biosynthesis. Pronounced inhibition of the incorporation of glycine-2-14C into the guanine and adenine nucleotides of the nucleic acids, coup...
Unnatural bases, 2-amino-6-(2-thienyl)purine and 2-amino-6-(2-furanyl)purine, were newly designed to replace the previously developed purine analogue, 2-amino-6-(N,N-dimethylamino)purine, which specifically pairs with pyridin-2-one. These nucleoside derivatives were synthesized via the 6-substit...
Reaction of 2,2′-diphthalimidodiethylamine with 2-vinylpyridine in H2O/MeOH and deprotection with HCl(aq) does not give the anticipated tripodal ligand N-2-(2-pyridylethyl)-N,N-bis(2-aminoethyl)amine. Instead, the new linear tetradentate tetraamine ligand N-{2-[(2-pyridin-2-ylethyl)amino]ethyl}...
For a series of benzaldehydes only with a leaving group or with both a leaving group and a single methoxy substituent 18F-fluorination via nucleophilic aromatic substitution (SNAr) was studied in DMF and Me2SO. In general, the radiochemical yields were clearly higher in DMF than in Me2SO. In the...
The formation of hydrogen-bonded complexes in the mixtures of 1,5,7-triazabicyclo[4.4.0]dec-5-ene (TBD) with 4-tert-butylphenol and 4-cyanophenol has been studied as a function of the phenol concentration in chloroform and acetonitrile by FTIR spectroscopy. In chloroform, the formation of cyclic...
The crystal structure of the 1:1 complex of lasalocid acid with 1,5,7-triazabicyclo[4.4.0]dec-5-ene (TBD) has been studied by X-ray diffraction, FT-IR spectroscopy and 1H NMR. The crystal space group is P212121 with a = 11.401(2) Å, b = 13.393(3) Å, c = 30.063(6) Å and Z = 4. In the crystal of t...
The normal coordinate analysis and calculation of the IR absorption band intensities have been carried out for 1,5,7-triazabicyclo[4,4,0]dec-5-ene (TBD) and its three possible protonated tautomeric forms. It has been shown that protonated molecule TBD has only one tautomeric species in which pro...
1,5,7-Triazabicyclo[4.4.0]dec-5-ene (TBD), a bicyclic guanidine base, has been found to be an excellent catalyst for Michael and Michael-type reactions. A wide variety of Michael donors and acceptors can participate in these reactions using 10–20 mol % of TDB. These reactions are mild, fast, ea...
The 1:1 complexes of 4-nitrophenyl[bis(diethylsulfonyl)]methane (CH1) and phenyl[bis(diethylsulfonyl)]methane (CH2) with 1,5,7-triazabicyclo[4.4.0]dec-5-ene (TBD) and 7-methyl-1,5,7-triazabicyclo[4.4.0]dec-5-ene (MTBD) have been synthesized and their structures have been studied using the FT-IR,...
The series of six carbon acids activated by two sulfonyl groups have been synthesized and the products of their deprotonation in acetonitrile solution by 1,5,7-triazabicyclo[4.4.0]dec-5-ene (TBD) were defined by electrospray ionization mass spectrometry method. The deprotonation of carbon acids ...
Immobilization of 1,5,7-triazabicyclo [4.4.0] dec-5-ene (TBD, a bicylic guanidine base) over mesoporous material like SBA-15 has been found to be an excellent catalyst for Michael-addition of β-nitro styrene with malonate. The reactions were performed under solvent-free condition at 373 K for 9...
Hydrogenation (3 atm) of readily available pyrido[1,2-a]pyrimidines 10, 14, and 17 over 5% Rh/Al2O3 forms 1,5-diazabicyclo[4.4.0]dec-5-enes 9, 15, and 18 in >95% yield, providing a general route to this little-studied class of compounds. All attempts to form the tetrahydro-1,2,4-triazine moiety ...
A novel water soluble phosphine, N,N-dipolyoxyethylene-substituted-4-(diphenylphosphino) benzenesulfonamide (PEO-DPPSA), is synthesized by ethoxylation of 4-(diphenylphosphino) benzenesulfonamide Ph2P–C6H4SO2NH2 (DPPSA) obtained from palladium-catalyzed P–C coupling reaction between 4-I–C6H4S...
A series of α-diimine nickel complexes bearing para-benzhydryl groups, {[(2,6-R2-4-CHPh2C6H2N = C)2Nap]NiBr2, Nap: 1,8-naphthdiyl, R = Me (C1); R = Et (C2); R = iPr (C3)}, were synthesized and characterized. Upon activation with AlEt2Cl, these para-benzhydryl substituted catalysts conducted the...
A study on the molecular structure and energetics of 10,11-dihydro-5H-dibenzo[a,d]cycloheptene (dibenzosuberane) was performed combining experimental calorimetric techniques and high level computational calculations. In the experimental work, the solid phase standard (p∘ = 0.1 MPa) molar enthal...
A series of novel 8-sulfonyl-substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles (THPI) has been synthesized and their ability to interact with 5-HT6 receptors evaluated in cell-based and radioligand binding assays. Amongst evaluated THPIs, compounds 9.HCl and 20.HCl have been identified as t...
Tissue cultures of the indigenous tree Nothapodytes foetida were established from immature embryos on Murashige and Skoog's agar medium supplemented with different auxins and cytokinins. The embryos developed unorganized callus tissues in medium containing BA + 2,4-D. BA + NAA medium promot...
9-Methoxycamptothecin (MCPT) has been recently reported to have a strong anticancer activity. However, its detailed mechanism of action in human cancer cells has not been well clarified. The results showed that MCPT induced cytotoxicity in seven human cancer cell lines in a dose dependent manner...
Camptothecin and 10-hydroxycamptothecin are two important precursors for the synthesis of the clinically useful anticancer drugs, topotecan and irinotecan. In recent years, efforts have been made to identify novel plant and endophytic fungal sources of camptothecin and 10-hydroxycamptothecin. In...
The electrochemical properties of 10-Hydroxycamptothecin were investigated systematically at a reduced graphene oxide modified glassy carbon electrode. A new pair of redox peaks of 10-Hydroxycamptothecin was reported for the first time with quasi-reversible process driven by adsorption. The dyna...
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