Design and synthesis of tetrazole tethered quinazoline derivatives via azide-isocyanide cross-coupling reaction: Exploring the utility as anticancer agents via the SRC kinase inhibition in breast cancer.

Kinases, particularly non-receptor tyrosine kinases (nRTK), are vital growth factors that determine the fate of numerous cancers, including breast cancer (BC). One such nRTK is c-Src, which plays a profound role in BC, is associated with BC development and metastasis, and induces resistance to cancer therapeutics. Considering the critical role of c-Src in BC outcome, we herein rationally designed and developed the tetrazole tethered quinazoline derivatives, considering the pharmacophoric feature of the catalytic domain of c-Src.

Pyrazole in drug development: a medicinal-chemistry based analysis of USFDA-approved drugs in last decade.

Among the diversity of existing heterocycles, nitrogen-containing heterocycles, i.e., azaheterocycles, are the most popular entity in drug discovery.

Access to Sterically Hindered Thioethers (α-Thioamides) Under Mild Conditions Using α-Halohydroxamates: Application toward 1,4-Benzothiazinones and 4,1-Benzothiazepinones.

Herein, we report a new and highly efficient approach for synthesizing congested α-thioamides under mild reaction conditions (mild base, room temperature, and short duration) using α-halo hydroxamates as direct alkylating agents. The reaction works well with both (hetero)aryl and alkyl thiols, tolerating a broad functional group and diverse substrate scope, including benzeneselenol for selenoether construction. The strategy enables efficient synthesis of biologically relevant 1,4 benzothiazinone and 4,1-benzothiazepinone cores, along with various other functionalized sulfur-based scaffolds of biological importance.

Correction: Pd-Catalysed [3 + 2]-cycloaddition towards the generation of bioactive bis-heterocycles/identification of COX-2 inhibitors analysis.

Correction for 'Pd-Catalysed [3 + 2]-cycloaddition towards the generation of bioactive bis-heterocycles/identification of COX-2 inhibitors analysis' by Elagandhula Sathish , , 2022, , 4746-4752, https://doi.org/10.1039/D2OB00467D.

Heteroarylation of Congested α-Bromoamides with Imidazo-Heteroarenes and Indolizines via Aza-Oxyallyl Cations: Enroute to Dibenzoazepinone and Zolpidem Analogues.

Herein, we report a highly efficient and unprecedented approach for heteroarylation of congested α-bromoamides via electrophilic aromatic substitution of imidazo-heteroarenes and indolizines under mild reaction conditions (room temperature, metal, and oxidant free). The participation of an in situ generated aza-oxyallyl cation as an alkylating agent is the hallmark of this transformation. The method was readily adapted to synthesize novel imidazo-heteroarene-fused dibenzoazepinone architectures of potential medicinal value.

Pd-Catalysed [3 + 2]-cycloaddition towards the generation of bioactive bis-heterocycles/identification of COX-2 inhibitors analysis.

In the current research, we envisaged the synthesis of bis-heterocycles containing the dihydroisoxazole ring by [3 + 2] cycloaddition of VECs (vinyl ethylene carbonates) and nitrile oxides, assisted by a Pd catalyst. Herein we explored hydroximoyl chlorides as versatile precursors for the generation of nitrile oxides that were exploited to achieve the cycloaddition reaction on a vinyl group of VECs to generate bis-heterocycles. -based studies of bis-heterocycles on the cyclooxygenase (COX) enzyme displayed selective COX-2 inhibition.

Metal free amination of congested and functionalized alkyl bromides at room temperature.

Herein, we report a highly facile and unprecedented approach to synthesize congested N-(hetero)aryl amines en route to α-amino acid amides using α-bromoamides as alkylating agents under mild reaction conditions (room temperature). The involvement of aza-oxyallyl cations as alkylating agents is the hallmark of this reaction. The method was readily adapted for the rapid synthesis of coveted 1,4-benzodiazepine-3,5-diones.