Design, synthesis, and in vitro and in vivo biological evaluation of 2-amino-naphtho[2,3-b]thiophene-4,9-dione derivatives as potent anticancer agents.

This study synthesized a series of substituted 2-amino-naphtho[2,3-b]thiophene-4,9-dione derivatives through multi-component reactions involving Domino and Krapcho strategies. Among the 15 synthesized analogs, compound 4a emerged as a lead compound with potent anticancer activity against the aggressive triple-negative breast cancer (TNBC) cell line MDA-MB-231. Mechanistic investigations demonstrated that treatment with compound 4a induced dose-dependent inhibition of cell viability, cell cycle arrest, and robust apoptotic responses in MDA-MB-231 cells.

Copper (II) Triflate/ Vitamin-C Promoted Modified Morita-Baylis-Hillman Annulation: A Facile Route to Fluorescent Cyclopentene Derivatives.

Herein we report a rapid and efficient method for the synthesis of fused cyclopentenoids via Intramolecular Morita-Baylis-Hillman (IMBH) annulation. In this approach, copper triflate (Cu(OTf)) serves as the promoter, favoring cyclization and aromatization over the conventional MBH addition product. A characteristic feature among most of the cyclized product contain two non-separable isomeric mixture of cyclopentene derivatives which has been readily interconverted via 1,5-H shift.

Progress in Electrochemically Empowered C-O Bond Formation: Unveiling the Pathway of Efficient Green Synthesis.

(C-X) bonds (X=C, N, O) are the main backbone for making different skeleton in the organic synthetic transformations. Among all the sustainable techniques, electro-organic synthesis for C-X bond formation is the advanced tool as it offers a greener and more cost-effective approach to chemical reactions by utilizing electrons as reagents. In this review, we want to explore the recent advancements in electrochemical C-O bond formation.

Urea-Promoted Neat Synthesis of Fused Dihydroisoquinolines and Disubstituted Pyridines: A Mechanistic Observation with Molecular-Sensing Studies.

An efficient and short synthesis of fused dihydroisoquinolines, diaryl substituted pyridine derivatives in good to high yields has been established by using an environmentally safe, solvent-metal-oxidant-free tandem approach. In this article, we discuss how the electrocyclic reaction is more pronounced in the solid phase in the presence of urea, whereas the typical aza-Michael addition is more prominent in presence of arylamine in the solution phase for 3-(2-formylcycloalkenyl)acrylic ester derivative substrates. The wide range of substrates and urea-promoted neat synthesis made our approach more significant in medical and also analytical science.

Synthesis of Multifused Pyrrolo[1,2-]quinoline Systems by Tandem Aza-Michael-Aldol Reactions and Their Application to Molecular Sensing Studies.

Herein, we have presented a weak acid-promoted tandem aza-Michael-aldol strategy for the synthesis of diversely fused pyrrolo[1,2-]quinoline (tricyclic to pentacyclic scaffolds) by the construction of both pyrrole and quinoline ring in one pot. The described protocol fabricated two C-N bonds and one C-C bond in the pyrrole-quinoline rings which have been sequentially formed under transition-metal-free conditions by the extrusion of eco-friendly water molecules. A ketorolac drug analogue has been synthesized following the current protocol, and one of the synthesized tricyclic pyrrolo[1,2-]quinoline fluorophores has been used to detect highly toxic picric acid via the fluorescence quenching effect.

One-pot tandem cyclisation to pyrrolo[1,2-a][1,4]benzodiazepines: a modified approach to the Pictet-Spengler reaction.

We have reported a one-pot two-step methodology for the synthesis of highly condensed heterocycles, pyrrolo[1,2-a][1,4]benzodiazepines, by a modified Pictet-Spengler reaction under mild conditions in a short time. Our approach has a few advantages over the conventional two components synthesis as it is step and atom economic, environmentally benign and a convergent synthetic method. We have discussed here the broad substrate scope of this novel methodology.

Intramolecular macrolactonization, photophysical and biological studies of new class of polycyclic pyrrole derivatives.

Herein, we report an efficient synthesis of N-substituted pyrrole derivatives and their application to construct macrocyclic oxazocinone via a two-component coupling reaction followed by base mediated intramolecular cyclization. This methodology provides an easy two-step approach to constitute a library of fused pyrrolo-oxazocinone derivatives in good yields under mild reaction conditions. The present methodology offers an easy access to the synthesis of a library of fluorescent pyrole derivatives.

Correction: Pyrido[1,2-a]pyrimidinium ions - a novel bridgehead nitrogen heterocycles: synthesis, characterisation, and elucidation of DNA binding and cell imaging properties.

Correction for 'Pyrido[1,2-a]pyrimidinium ions - a novel bridgehead nitrogen heterocycles: synthesis, characterisation, and elucidation of DNA binding and cell imaging properties' by Susanta Kumar Manna et al., Org. Biomol.

Pyrido[1,2-a]pyrimidinium ions--a novel bridgehead nitrogen heterocycles: synthesis, characterisation, and elucidation of DNA binding and cell imaging properties.

A novel class of bridgehead nitrogen heterocycles, pyrido[1,2-a]pyrimidinium ions, has been readily synthesized by a two-step one-pot reaction in high yields (up to 93%). These ionic compounds are bench stable and moisture tolerant and have highly fluorescent properties (quantum yield up to 0.65).

Novel and rapid palladium-assisted 6pi electrocyclic reaction affording 9,10-dihydrophenanthrene and its analogues.

A novel methodology for the synthesis of 9,10-dihydrophenanthrene and its analogues has been developed via a palladium-assisted 6pi electrocyclic reaction followed by formaldehyde elimination.