87273-75-4Relevant academic research and scientific papers
Characterization of new Pt(IV)–thiazole complexes: Analytical, spectral, molecular modeling and molecular docking studies and applications in two opposing pathways
Althagafi, Ismail,El-Metwaly, Nashwa M.,Farghaly, Thoraya
, (2019/08/12)
New thiazole derivatives were synthesized and fully characterized, then coordinated with PtCl4 salt. Also, the newly synthesized Pt(IV) complexes were investigated analytically (elemental and thermogravimetric analyses), spectrally (infrared, UV–visible, mass, 1H NMR, 13C NMR, X-ray diffraction) as well as theoretically (kinetics, modeling and docking). The data extracted led to the establishment of the best chemical and structural forms. Octahedral geometry was the only formula proposed for all complexes, which is favorable for d6 systems. The molecular ion peaks from mass spectral analysis coincide with all analytical data, confirming the molecular formula proposed. X-ray diffraction (XRD) and scanning electron microscopy (SEM) allowed discrimination of features between crystalline particles and other amorphous morphology. By applying Gaussian09 as well as HyperChem 8.2 programs, the best structural forms were obtained, as well as computed significant parameters. Computed parameters such as softness, hardness, surface area and reactivity led us towards application in two opposing pathways: tumor inhibition and oxidation activation. The catalytic oxidation for CO was conducted over PtO2, which was yielded from calcination of the most reactive complex. The success of catalytic role for synthesized PtO2 was due to its particulate size and surface morphology, which were estimated from XRD patterns and SEM images, respectively. The antitumor activity was tested versus HCT-116 and HepG-2 cell lines. Mild toxicity was recorded for two of the derivatives and their corresponding complexes. This degree of toxicity is more favorable in most cases, due to exclusion of serious side effects, which is coherently attached with known antitumor drugs.
Efficient synthesis of new functionalized 2-(hetaryl)thiazoles
Bondock, Samir,El-Azab, Hossam,Kandeel, Ez-Eldin M.,Metwally, Mohamed A.
, p. 59 - 71 (2012/11/06)
An efficient synthesis of the hitherto unknown ring system, 2-heteroaryl-thiazoles, is described via the reaction of 3-oxo-N-(4- phenylthiazol-2-yl)butanamide (1) with diazotized heterocyclic amine, phenyl isothiocyanate, dimethylformamide-dimethylacetal,
S-PHENACYLATION OF 6-METHYL-4-OXO-2-THIO-2,3-DIHYDRO-4H-1,3-OXAZINE AND THE RING TRANSFORMATION OF THE S-PHENACYLATED COMPOUND
Sasaki, Tadashi,Ito, Eikoh,Asai, Koji
, p. 1089 - 1097 (2007/10/02)
1,3-oxazine 1 reacted with phenacyl bromide in water using sodium hydroxide as a base to give S-phenacylated derivative 2, but the homogeneous conditions such as NaH in THF or NaOMe in methanol caused the base-induced cycloreversion of 1, resulting in the formation of thiocyanate 3.For the purpose of the intramolecular transformation to pyrimidine-fused heterocycle 11, 2 was treated with ammonia in refluxing ethanol, but gave amidamine 6 while 8 was obtained with ammonium acetate in refluxing acetic acid.Although the direct ring closure failed, the target 11 was finally synthesized by the cyclodehydration of ketamide 7 with phosphorus pentoxide at 250 deg C.
