Abdallah Hamzé
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View article: Mechanochemical Approach for Metal‐Free Regioselective C5‐Sulfenylation of Imidazo[2,1‐<i>b</i>]Thiazoles
Mechanochemical Approach for Metal‐Free Regioselective C5‐Sulfenylation of Imidazo[2,1‐<i>b</i>]Thiazoles Open
The development of sustainable and selective methodologies for heterocyclic functionalization remains a key challenge in organic synthesis. In this study, a novel, metal‐free bis(trifluoroacetoxy)iodo]benzene‐mediated strategy for the regi…
View article: Illuminating the Path of Rearrangement: Visible Light‐Driven Pd‐Catalyzed Substituted Olefins Synthesis
Illuminating the Path of Rearrangement: Visible Light‐Driven Pd‐Catalyzed Substituted Olefins Synthesis Open
Pd‐catalyzed reactions are among the most straightforward and efficient methods to proficiently build Csp 2 ‐Csp 2 bonds. Nevertheless, thermal activation remains mandatory in most cases, which may decrease the compatibility with sensitive…
View article: Copper‐Catalyzed Domino Synthesis of Spiropyrazoline Oxindoles via Condensation of Indolin‐2‐One and Phenylhydrazine Derivatives
Copper‐Catalyzed Domino Synthesis of Spiropyrazoline Oxindoles via Condensation of Indolin‐2‐One and Phenylhydrazine Derivatives Open
We report a straightforward and efficient method for the synthesis of spiropyrazoline oxindoles using CuCl 2 as the Lewis acid catalyst. This approach involves a one‐pot domino process, consisting of a condensation step between indolin‐2‐o…
View article: Recent Advancements in the Development of HDAC/Tubulin Dual-Targeting Inhibitors
Recent Advancements in the Development of HDAC/Tubulin Dual-Targeting Inhibitors Open
Histone deacetylases (HDACs) have become one of the main targets in cancer therapy due to their involvement in various biological processes, including gene regulation, cell proliferation, and differentiation. Microtubules, as key elements …
View article: Recent Advancements in the Development of HDAC/Tubulin Dual-Targeting Inhibitors
Recent Advancements in the Development of HDAC/Tubulin Dual-Targeting Inhibitors Open
Histone deacetylases (HDACs) become one of the main targets in cancer therapy due to their involvement in various biological processes, including gene regulation, cell proliferation and differentiation. On the other hand, microtubules as k…
View article: Dual molecule targeting HDAC6 leads to intratumoral CD4+ cytotoxic lymphocytes recruitment through MHC-II upregulation on lung cancer cells
Dual molecule targeting HDAC6 leads to intratumoral CD4+ cytotoxic lymphocytes recruitment through MHC-II upregulation on lung cancer cells Open
Background Despite the current therapeutic treatments including surgery, chemotherapy, radiotherapy and more recently immunotherapy, the mortality rate of lung cancer stays high. Regarding lung cancer, epigenetic modifications altering cel…
View article: Overcoming Solubility Challenges: Liposomal isoCoQ‐Carbazole as a Promising Anti‐Tumor Agent for Inoperable and Radiation‐Insensitive cancers
Overcoming Solubility Challenges: Liposomal isoCoQ‐Carbazole as a Promising Anti‐Tumor Agent for Inoperable and Radiation‐Insensitive cancers Open
This study evaluated the potential of iso CoQ‐Carbazole, a diheterocyclic analog of iso CA‐4, as an anti‐tumor agent. To overcome its low aqueous solubility, liposomes were developed as a delivery system for the compound. In vitro experime…
View article: Mo-catalyzed cyclization of <i>N</i>-vinylindoles and skatoles: synthesis of dihydroindolo[1,2-<i>c</i>]-quinazolines and dihydroindolo[3,2-<i>b</i>]-indoles, and evaluation of their anticancer activities
Mo-catalyzed cyclization of <i>N</i>-vinylindoles and skatoles: synthesis of dihydroindolo[1,2-<i>c</i>]-quinazolines and dihydroindolo[3,2-<i>b</i>]-indoles, and evaluation of their anticancer activities Open
Unveiling a Mo-catalyzed synthesis, unprecedented anticancer dihydroindolo[1,2- c ]-quinazolines and dihydroindolo[3,2- b ]-indoles were discovered from N -vinylazoles.
View article: Leveraging <i>in situ N</i>-tosylhydrazones as diazo surrogates for efficient access to pyrazolo-[1,5-<i>c</i>]quinazolinone derivatives
Leveraging <i>in situ N</i>-tosylhydrazones as diazo surrogates for efficient access to pyrazolo-[1,5-<i>c</i>]quinazolinone derivatives Open
We developed a transition metal-free methodology for the construction of pyrazoloquinazolinone derivatives.
View article: Overcoming Solubility Challenges: Liposomal isoCoQ-Carbazole as a Promising Anti-Tumor Agent for Inoperable and Radiation-Insensitive Cancers
Overcoming Solubility Challenges: Liposomal isoCoQ-Carbazole as a Promising Anti-Tumor Agent for Inoperable and Radiation-Insensitive Cancers Open
This study evaluated the potential of isoCoQ-Carbazole, a diheterocyclic analog of isoCA-4, as an anti-tumor agent. To address its low aqueous solubility, liposomes were developed as a delivery system for the compound. In vitro experiments…
View article: Synthesis of Aza‐Heterocyclic Compounds with <i>N</i>‐Tosylhydrazones: Formation of Bi‐Indoles via Reductive Molybdenum Catalysis
Synthesis of Aza‐Heterocyclic Compounds with <i>N</i>‐Tosylhydrazones: Formation of Bi‐Indoles via Reductive Molybdenum Catalysis Open
In this study, we present a methodology for synthesizing aza‐heterocyclic compounds using N ‐tosylhydrazones as key reagents. Our primary objective was to obtain six or seven‐membered ring heterocycles; however, we unexpectedly observed th…
View article: CCDC 2240365: Experimental Crystal Structure Determination
CCDC 2240365: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 2240364: Experimental Crystal Structure Determination
CCDC 2240364: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Recent Advances in Synthesis of Pyrrolo[3,2‐<i>b</i>]indole and Indolo[3,2‐<i>b</i>]indole Derivatives
Recent Advances in Synthesis of Pyrrolo[3,2‐<i>b</i>]indole and Indolo[3,2‐<i>b</i>]indole Derivatives Open
During the last 15 years, many teams have developed new accesses to pyrrolo[3,2‐ b ]indoles, indolo[3,2‐ b ]indoles, and polycyclic counterparts for finding either new synthetic pathways or their electronic and photochromic properties. In …
View article: Recent Developments in the Photochemical Synthesis of Functionalized Imidazopyridines
Recent Developments in the Photochemical Synthesis of Functionalized Imidazopyridines Open
Imidazopyridines constitute one of the most important scaffolds in medicinal chemistry, as their skeleton could be found in a myriad of biologically active molecules. Although numerous strategies were elaborated for imidazopyridine prepara…
View article: High-Throughput Screening for Extracellular Inhibitors of the FLT3 Receptor Tyrosine Kinase Reveals Chemically Diverse and Druggable Negative Allosteric Modulators
High-Throughput Screening for Extracellular Inhibitors of the FLT3 Receptor Tyrosine Kinase Reveals Chemically Diverse and Druggable Negative Allosteric Modulators Open
Inhibiting receptor tyrosine kinases is commonly achieved by two main strategies targeting either the intracellular kinase domain by low molecular weight compounds or the extracellular ligand-binding domain by monoclonal antibodies. Identi…
View article: Recent Progress on the Mild Deprotection of Dithioketals, Dithioacetals, and Oxathiolanes
Recent Progress on the Mild Deprotection of Dithioketals, Dithioacetals, and Oxathiolanes Open
Reactions for the deprotection of carbonyl derivatives have been of considerable interest to the scientific community. In recent years efforts have been made to develop mild, experimentally simple, and environmentally friendly methods. Thi…
View article: Synthesis and Biological Activities of Pyrazino[1,2-a]indole and Pyrazino[1,2-a]indol-1-one Derivatives
Synthesis and Biological Activities of Pyrazino[1,2-a]indole and Pyrazino[1,2-a]indol-1-one Derivatives Open
This review concerns the synthesis and biological activities of pyrazino[1,2-a]indoles and pyrazino[1,2-a]indol-1-ones reported since 1997 and the discovery of biological activity of pyrazinoindole derivatives. In the first part, we first …
View article: Recent advances in the synthesis of pyrido[1,2-<i>a</i>]indoles
Recent advances in the synthesis of pyrido[1,2-<i>a</i>]indoles Open
This review deals with the different accesses leading to the pyrido[1,2-a]indole nucleus in the last 20 years.
View article: Mild Deprotection of Dithioacetals by TMSCl/NaI Association in CH <sub>3</sub> CN
Mild Deprotection of Dithioacetals by TMSCl/NaI Association in CH <sub>3</sub> CN Open
A mild process using a combination of TMSCl and NaI in acetonitrile is used to regenerate carbonyl compounds from a variety of dithiane and dithiolane derivatives. This easy to handle and inexpensive protocol is also efficient to deprotect…
View article: Mild Deprotection of Dithioacetals by TMSCl / NaI Association in CH3CN
Mild Deprotection of Dithioacetals by TMSCl / NaI Association in CH3CN Open
We showed for the first time, the fundamental role of CH 3 CN associated to TMSCl/NaI combination to deprotect S,S-ethylene- and S,S-propylene-ketals into ketones. Indeed, if the TMSCl/NaI association leads to the reduction of dithioketals…
View article: Mild Deprotection of Dithioacetals by TMSCl / NaI Association in CH3CN
Mild Deprotection of Dithioacetals by TMSCl / NaI Association in CH3CN Open
We showed for the first time, the fundamental role of CH3CN associated to TMSCl/NaI combination to deprotect S,S-ethylene- and S,S-propylene-ketals into ketones. Indeed, if the TMSCl/NaI association leads to the reduction of dithioketals i…
View article: How do we improve histone deacetylase inhibitor drug discovery?
How do we improve histone deacetylase inhibitor drug discovery? Open
KEYWORDS: Histone deacetylasehistone deacetylase inhibitorscancerdrugs combinationmultitargeted drugs