Deoxycytidine kinase (dCK, EC.2.7.1.74) is a key enzyme in the intracellular metabolism of 2-chlorodeoxyadenosine, 1-β-d-arabinofuranosylcytosine, difluorodeoxycytidine, and other drugs used in chemotherapy of different leukaemias and solid tumours. Recently, stimulation of dCK activity was sho...

Bolus doses of 5-chlorodeoxycytidine (CldC) administered with modulators of pyrimidine metabolism, followed by X-irradiation, resulted in a 2-fold dose increase effect against RIF-1 tumors in C3H mice. Pool size studies of the fate of [14-C]-CldC in BDF1 mice bearing Sarcoma-180 tumors, which de...

DNA methylation of the CpG-rich 5′ region of the deoxycytidine kinase (dCK) gene is potentially involved in the suppression of the gene and the resistance of tumour cells to arabinosylcytosine (ara-C). 2-Chlorodeoxyadenosine (cladribine, CdA) and 2-chloro-2′-arabino-fluoro-2′-deoxyadenosine (...

5-Chloro-2′-deoxycytidine (CIdC) + tetrahydrouridine (H4U) sensitizes mammalian cells (HEp-2, RIF-1, 5-180) to X ray. This sensitization, as demonstrated previously with HEp-2 cells, is heightened when cells are pre-incubated with inhibitors of pyrimidine synthesis. CHO cells, which intrinsical...

Deoxycytidine kinase (dCK, EC.2.7.1.74), a key enzyme in intracellular metabolism of many antileukemic drugs, was shown to be activated during treatment of lymphocytes by 2-chloro-2′-deoxyadenosine (Cl-dAdo, cladribine), a potent inhibitor of DNA synthesis. While 5-[3H]-thymidine (TdR) incorpor...

5-Chloro-2′-deoxycytidine (NSC 371331, CDC) is in development as a possible radiosensitizing agent for cancer treatment. Previous studies have been done to demonstrate the in vivo efficacy of CDC with various modulators of its metabolism. This paper describes our preclinical studies to determin...

Three novel donor-acceptor type organic semiconductors PO1TPA, PO2TPA, and 2POTPA composed of arylamine donor and arylphosphine oxide acceptor were designed and synthesized through ortho-linking strategy. By varying the donor/acceptor ratio in these compounds, the effect of donor-acceptor connec...

Two novel small-molecules PO-PhQ and PO-PhQNO, in which both polar phosphine oxide (PO) and N–oxide (NO) groups are incorporated in phenyl quinolone core unit were synthesized as efficient cathode interfacial layers (CILs) for inverted organic solar cells (IOSCs). Because of the phenylquinoline...

High triplet energy host materials based on novel fused phenylcarbazole core structure and diphenylphosphine oxide were synthesized and the physical properties of the host materials were investigated. A high triplet energy of 2.95 eV was obtained from the fused phenylcarbazole based host materia...

Aroyl group driven phosphonate-phosphate rearrangement in dialkyl/aryl(α-hydroxy-β-oxo-β-arylethyl)phosphonates having α-proton under basic conditions is presented and extended to a novel one-pot direct coupling method between 2-oxoaldehydes (2OA) and H-phosphonates/diphenylphosphine oxide. ...

A novel electron transport material with 1,2,4-triazole and diphenylphosphine oxide moieties (TPO) has been designed and synthesized. The material exhibits wide energy gap (3.77 eV), deep HOMO level (−6.28 eV), high triplet energy (2.86 eV), high glass transition temperature (133 °C) and high t...

An asymmetric Michael addition of diphenylphosphine to β,γ-unsaturated α-keto esters was developed using a P-stereogenic pincer-Pd complex as a catalyst. The corresponding hydrophosphination products were obtained in good yields (up to 94%) and with moderate to good enantioselectivities (up t...

A series of high triplet energy host materials with a carbazole core and a diphenylphosphine oxide substituent were synthesized and the effect of the substitution position on the photophysical properties and device performances of the host material was investigated. The substitution position of ...

Three novel host materials based on carbazole (Cz) and diphenylphosphine oxide (DPPO) by the different linkages method were designed and synthesized, named (3'-(9H-carbazol-9-yl)-[1,1′-biphenyl]-4-yl)diphenylphosphine oxide (CzPhPO), (4-(9-phenyl-9H-carbazol-2-yl)phenyl) diphenylphosphine ...

Two novel host materials based on the diphenylphosphine oxide (DPPO) and spirofluorene were designed and facilely synthesized by tuning the ratio of donor spirofluorene units and acceptor DPPO units from 1: 1 to 1: 2, i. e., (4-(9,9′-spirobi[fluoren]-2-yl)phenyl)diphenylphosphine oxide (SPDPPO)...

A new method for the synthesis of thiophosphates by reductive coupling reaction of diphenylphosphine oxide and sulfonyl chlorides has been developed. The reaction is metal-free and needs no additives, affording various aryl and alkyl substituted thiophosphates in good to excellent yields under m...

An efficient procedure for the synthesis of (20S)-3β-acetoxy-5α-pregnane-20,16β-carbolactone is described. Bactericidal and fungicidal activity of the lactone against different bacteria such as MSSA, MRSA, E. coli ESBL, P. aeruginosa and clinical isolates of Candida spp., in planktonic and bi...

The reaction of phenylacetamides with oxalyl chloride/Lewis acid provides a convergent, high-yield entry to C-homoprotoberberine and 8-oxoprotoberberine alkaloids from available starting materials. This approach was used to synthesize 8-oxopseudopalmatine starting from N-[β-(3′,4′-dimethoxyph...

In the present study, the mechanism of antiplatelet activity of DK-002, a synthesized (6aS,cis)-9,10-Dimethoxy-7,11b-dihydro-indeno[2,1-c]chromene-3,6a-diol, was investigated. DK-002 inhibited the thrombin, collagen, and ADP-induced rat platelet aggregation in a concentration-dependent manner, w...

Metal complexes of the 2,4-di-t-butyl-1,3-diphosphacyclobutadiene ligand have been synthesized by head-to-tail dimerization of t-BuCP: on transition metal sites. In this connection the geometries and energetics of the complete series of binuclear cobalt carbonyl complexes (Me2C2P2)2Co2(CO)n (n =...