Design, synthesis, docking study, and anticancer evaluation of novel bis-thiazole derivatives linked to benzofuran or benzothiazole moieties as PI3k inhibitors and apoptosis inducers

Radwan, Ibrahim Taha; Elwahy, Ahmed H. M.; Darweesh, Ahmed F.; Sharaky, Marwa; Bagato, Noha; Khater, Hanem F.; Salem, Mostafa E.

doi:10.1016/j.molstruc.2022.133454

Cited by 22 publications

(14 citation statements)

References 74 publications

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“…The FTIR spectrum of free ligand (HMABP) exhibited a strong bands at (1600) cm -1 and at (1575) cm -1 which were assigned to ʋ(C=N) groups vibrations of azomethine and benzothiazole ring respectively (34) , these bands were shifted to lower frequencies with noticeable change in their shape in the spectra of all the complexes (35) . These differences are considered a good indicator for coordination of the metal ions with nitrogen atom of azomethine and benzothiazole ring.…”

Section: Ir Spectra Of Ligands and Complexesmentioning

confidence: 99%

Synthesis, spectral properties and antibacterial studies of new hetrocyclic schiff-azo ligand derived from 5-amino 2-phenyl.4h-pyrazol-3-one with some transition metal complexes

Mohammed¹,

Wadday

2022

ijhs

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In this article, a synthesized ligand [5-amino 2-phenyl.4H-pyrazol-3-one ] and it was used to prepare new complexes of Mn (II),Co(II), Ni(II), Cu(II), Zn(II), Pd(II) and Ag(I). The new ligand (HMABP) has categorized by Micro Elemental Analysis (C.H.N.S), UV-visible, Fourier Transform infrared (FTIR) approaches, 1H,13C-NMR spectroscopy and mass spectroscopy. The consequence has specified that the ligand was represented as N,N,O-tetradentate. The preparing of complexes has accomplished after fixing the finest concentration and pH. UV-Vis spectra of these complexes solutions have been examined for a range of pH (3-10) and concentration (1x10-4-5.5x10-4) Molar that comply with Lambert-Beers Law. A stoichiometry of the complexes has comprehended in relation to mole ratio which has gotten from spectroscopic investigations of the complex has solutions. The ratio of metal: ligand was achieved with (1:1) for all complexes. The metal ions complexes were characterized by FTIR, UV-Visible, molar conductance, atomic absorption, magnetic susceptibility, elemental analysis C.H.N.S techniques. From the results of physico-chemical and spectral techniques, octahedral geometry except with Pd2+ was square planar and tetrahedral shape with Ag+ have been proposed for these metal complexes.

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Section: Ir Spectra Of Ligands and Complexesmentioning

confidence: 99%

Synthesis, spectral properties and antibacterial studies of new hetrocyclic schiff-azo ligand derived from 5-amino 2-phenyl.4h-pyrazol-3-one with some transition metal complexes

Mohammed¹,

Wadday

2022

ijhs

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“…Thiazole-containing drugs have anticancer action through a variety of pathways. [30][31][32][33][34][35] Based on the above-mentioned potential qualities and continue of our previous work, [36][37][38][39][40] the study's strategy included combining of the two bioactive substances pyrazole and thiazole into a single compact structure for synergism and assessing the resulting compounds as anticancer medicines.…”

Section: Introductionmentioning

confidence: 99%

“…Thiazole containing drugs, on the other hand, have been shown to be involved in a variety of commercially available anti‐cancer medications, including tiazofurin [ I ] (inhibitor of IMP dehydrogenase), [25] dasatinib [ II ] (Bcr−Abl tyrosine kinase inhibitor), [26] dabrafenib [ III ] (inhibitor of enzyme B−RAF), [27] ixabepilone [ IV ] (microtubule stabilisation) [28] andepothilone[ V ](inhibition of microtubule function) [29] (Figure 1). Thiazole‐containing drugs have anticancer action through a variety of pathways [30–35] …”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis, Cytotoxic Activity and Molecular Docking Studies of Naphthyl Pyrazolyl Thiazole Derivatives as Anticancer Agents

et al. 2023

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Novel series of heterocycliccompounds pairing hybrids pyrazole, naphthalene and pyrazoline/thiazoldinemoieties were synthesized. The starting compounds pyrazolyl hydrazinecarbothioamidewere synthesized by the reaction of the 4‐formyl pyrazole derivatives with thiosemicarbazide to afford the substituted carbothioamide in good yields. The carbothioamideswere used as starting materials for synthesis of a variety of pyrazolylhydrazinylthiazole derivativesandpyrazolylhydrazonothiazolidin derivatives. The structures of the newly synthesized compounds were deduced depending on their spectrum data and elemental analysis. The cytotoxicity of the selected compounds was screened in vitro against three human breast cancer cell lines. The four compounds showed a gradual decrease in cell viability and theonly compound thiazolidin‐4‐one10b showed IC5010.16, 8.25 and 4.88 μM against the above cell lines, respectively. Thus, it was selected for further in vitro biological investigations. The Structure‐activity relationship for these compounds was interpreted in terms of molecular docking.

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“…Also, the anticancer and kinase inhibitory activity of bisthiazole compounds is well established. 38,39 Inspired by these ndings, bisthiazole compound 15 was also synthesized to study the effect of dimerization on B-RAFV600E inhibition.…”

Section: Introductionmentioning

confidence: 99%

Novel thiazole derivatives incorporating phenyl sulphonyl moiety as potent BRAFV600E kinase inhibitors targeting melanoma

et al. 2022

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Design, synthesis, docking study, and anticancer evaluation of novel bis-thiazole derivatives linked to benzofuran or benzothiazole moieties as PI3k inhibitors and apoptosis inducers

Cited by 22 publications

References 74 publications

Synthesis, spectral properties and antibacterial studies of new hetrocyclic schiff-azo ligand derived from 5-amino 2-phenyl.4h-pyrazol-3-one with some transition metal complexes

Synthesis, spectral properties and antibacterial studies of new hetrocyclic schiff-azo ligand derived from 5-amino 2-phenyl.4h-pyrazol-3-one with some transition metal complexes

Design, Synthesis, Cytotoxic Activity and Molecular Docking Studies of Naphthyl Pyrazolyl Thiazole Derivatives as Anticancer Agents

Novel thiazole derivatives incorporating phenyl sulphonyl moiety as potent BRAFV600E kinase inhibitors targeting melanoma

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