The Effect of Actinomycin D on a Spectrum of Tumors*

Sugiura, Kanematsu

doi:10.1111/j.1749-6632.1960.tb20160.x

Cited by 24 publications

(8 citation statements)

References 7 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Pyrimidine moiety is one of the important classes of N-containing heterocycles widely used as key building blocks for pharmaceutical agents. It exhibits a wide spectrum of pharmacophore such as bactericidal, fungicidal, analgesic, anti-hypertensive and anti-tumor agents [10] , [11] , [12] , [13] . In addition, preclinical data from literature survey indicate continuing research in polysubstituted pyrimidine as potential anti-tumor agents [14] .…”

Section: Introductionmentioning

confidence: 99%

Spectroscopic analysis on the binding interaction of biologically active pyrimidine derivative with bovine serum albumin

Suryawanshi

Walekar

Gore

et al. 2016

Journal of Pharmaceutical Analysis

311

135

View full text Add to dashboard Cite

A biologically active antibacterial reagent, 2–amino-6-hydroxy–4–(4-N, N-dimethylaminophenyl)-pyrimidine-5-carbonitrile (AHDMAPPC), was synthesized. It was employed to investigate the binding interaction with the bovine serum albumin (BSA) in detail using different spectroscopic methods. It exhibited antibacterial activity against Escherichia coli and Staphylococcus aureus which are common food poisoning bacteria. The experimental results showed that the fluorescence quenching of model carrier protein BSA by AHDMAPPC was due to static quenching. The site binding constants and number of binding sites (n≈1) were determined at three different temperatures based on fluorescence quenching results. The thermodynamic parameters, enthalpy change (ΔH), free energy (ΔG) and entropy change (ΔS) for the reaction were calculated to be 15.15 kJ/mol, –36.11 kJ/mol and 51.26 J/mol K according to van't Hoff equation, respectively. The results indicated that the reaction was an endothermic and spontaneous process, and hydrophobic interactions played a major role in the binding between drug and BSA. The distance between donor and acceptor is 2.79 nm according to Förster's theory. The alterations of the BSA secondary structure in the presence of AHDMAPPC were confirmed by UV–visible, synchronous fluorescence, circular dichroism (CD) and three-dimensional fluorescence spectra. All these results indicated that AHDMAPPC can bind to BSA and be effectively transported and eliminated in the body. It can be a useful guideline for further drug design.

show abstract

Section: Introductionmentioning

confidence: 99%

Spectroscopic analysis on the binding interaction of biologically active pyrimidine derivative with bovine serum albumin

Suryawanshi

Walekar

Gore

et al. 2016

Journal of Pharmaceutical Analysis

311

135

View full text Add to dashboard Cite

show abstract

“…The 3,4-dihydropyrimidine and its derivatives are highly significant because they generally show diverse medicinal properties, such as calcium channel blockers, antihypertensive and anti-inflammatory agents, and α 1-a antagonists [8][9][10][11]. Furthermore, 3,4-dihydropyrimidine derivatives have emerged as important target molecules because of their pharmacological and therapeutic properties, such as antimitotic, antiviral, antitumor, anticarcinogenic, antibacterial, and fungicidal activities [12][13][14][15][16][17][18][19].…”

Section: Introductionmentioning

confidence: 99%

Green High-Yielding One-Pot Approach to Biginelli Reaction under Catalyst-Free and Solvent-Free Ball Milling Conditions

2016

View full text Add to dashboard Cite

A simple, green, and efficient approach was used to synthesize 3,4-dihydropyrimidines derivatives. We showed that the application of the planetary ball milling method with a ball-to-reagent weight ratio of 8 for the Biginelli reaction provides 3,4-dihydropyrimidines derivatives with excellent yields (>98%) in a short reaction time from the one-pot, three-component condensation of aldehydes, ethyl acetoacetate, and urea (or thiourea).

show abstract

“…They are components of nucleic acids. The important pyrimidine compounds have diverse applications as anti-bacterial (Pershin et al,1972), fungicidal (Metolcsy,1971), analgesics (Regnier et al, 1972), anti-inflammatory (Winter et al,1962) and anti-tumor agents (Suguira et al,1973). Nowadays the one step method involving three component condensation using different reagents (Dipti et al, 2010) are popular in synthetic organic chemistry for the synthesis of heterocyclic compounds.They are present in nature and are of great significance to life because their structural subunits exist in many natural products such as vitamins, hormones, antibiotics (Yuhong and Varma, 2006).…”

Section: Introductionmentioning

confidence: 99%