Recent synthetic strategies of small heterocyclic organic molecules with optoelectronic applications: a review.

Over the past few years, there have been tremendous developments in the design and synthesis of organic optoelectronic materials with appealing applications in device fabrication of organic light-emitting diodes, superconductors, organic lasers, organic field-effect transistors, clean energy-producing organic solar cells, etc. There is an increasing demand for the synthesis of green, highly efficient organic optoelectronic materials to cope with the issue of efficiency roll-off in organic semiconductor-based devices. This review systematically summarized the recent progress in the design and synthesis of small organic molecules having promising optoelectronic properties for their potential applications in optoelectronic devices during the last 10-year range (2010-early 2021).

Recent advances in the green synthesis of Betti bases and their applications: a review.

Well-known Betti bases are the products obtained by the one-pot multicomponent reaction of 1-naphthol/2-naphthol, aliphatic/aromatic aldehydes, and secondary amines, and this reaction is known as the Betti reaction. During recent years, due to the unveiling of the pharmacological and synthetic potential of Betti bases, a tremendous increase in the studies reporting novel synthetic methods for the efficient synthesis of Betti bases was observed. This review presents the recent key developments in the green synthesis of the Betti bases and accounts for the significant number of the literature reported during 2019-2022. Both catalyst free as well as the catalyst promoted synthesis (nanocatalyst, biocatalyst, transition metal catalyst, etc.) along with the synthetic applications (catalyst, ligands/chiral auxiliaries, and valuable synthons), optoelectronic applications (fluorescence sensors for phosgene gas, Hg2+, and Cr3+ detection, quasi-reversible redox potential) and biological properties (anticancer agents, antioxidant, anti-inflammatory agents, antitubercular agents, pesticidal agents, anti-Alzheimer agents, Topoisomerase I inhibitors, YAP-TEAD interaction inhibitors, and DNA binding and cleavage activity) are discussed. There is a surge of interest for the development of the green and efficient Betti reaction for the construction of C-C and C-N bond in a single-step reaction accessing Betti bases as products. Along with key methodological developments for the green synthesis of Betti bases, their applications in synthetic organic chemistry, optoelectronic sensors, advanced materials synthesis, agrochemicals and pharmaceutically active scaffolds, during the period of 2019-2022, have been considered.

Pharmacological potential of micheliolide: A focus on anti-inflammatory and anticancer activities.

Micheliolide (MCL) is a chief constituent of plants such as Magnolia grandiflora L., Michelia compressa (Maxim.) Sarg. and Michelia champaca L. It is known to exhibit significant anticancer activity by various scientific investigations. This review aims to emphasize the anticancer and antiinflammatory activities of MCL. In this review, we summarized the published data in peer-reviewed manuscripts published in English. Our search was based on the following scientific search engines and databases: Scopus, Google Scholar, ScienceDirect, Springer, PubMed, and SciFinder, MCL possesses a broad spectrum of medicinal properties like other sesquiterpene lactones. The anticancer activity of this compound may be attributed to the modulation of several signaling cascades (PI3K/Akt and NF-κB pathways). It also induces apoptosis by arresting the cell cycle at the G1/G0 phase, S phase, and G2/M phase in many cancer cell lines. Very little data is available on its modulatory action on other signaling cascades like MAPK, STAT3, Wnt, TGFß, Notch, EGFR, etc. This compound can be potentiated as a novel anticancer drug after thorough investigations in vitro, in vivo, and in silico-based studies.

Ring forming transformations of ynamides via cycloaddition.

Ynamides are N-alkyne compounds bearing an electron withdrawing group at the nitrogen atom. They offer unique pathways for the construction of versatile building blocks owing to their exceptional balance between reactivity and stability. Recently several studies have been reported that explore and illustrate the synthetic potential of ynamides and ynamide-derived advanced intermediates in cycloadditions with different reaction partners to yield heterocyclic cycloadducts of synthetic and pharmaceutical value. Cycloaddition reactions of ynamides are the facile and preferable routes for the construction of structural motifs having striking importance in synthetic, medicinal chemistry, and advanced materials. In this systematic review, we highlighted the recently reported novel transformations and synthetic applications that involved the cycloaddition reaction of ynamides. The scope along with the limitations of the transformations are discussed in detail.

Revisiting the Synthesis of Betti Bases: Facile, One-pot, and Efficient Synthesis of Betti Bases Promoted by FeCl3•6H2O.

BACKGROUND: Betti bases are pharmaceutically and synthetically important scaffolds due to their diverse range of biological activities and applications in key synthetic transformations in organic synthesis. OBJECTIVE: This work has been sought to contribute to the development, design, and implementation of an improved green methodology with higher atom economy and lower E-factor values for the synthesis of Betti bases. METHODS: To realize our objectives, we screened out different catalysts and reaction conditions using one-pot multicomponent modified Mannich reaction/Betti reaction by employing 2-naphthol, benzaldehyde and pyrrolidine as model substrates. RESULTS: The developed methodology afforded functionalized Betti bases in 60-100% yields via FeCl3•6H2O catalyzed one-pot multi-component Betti reaction under neat conditions at 110 °C (5-15 min) using several aromatic aldehydes and secondary amines. CONCLUSION: A facile synthetic methodology with higher atom economy and lower E-factor values to synthesize Betti bases via FeCl3•6H2O catalyzed one-pot multicomponent Betti reaction of 2-naphthol, aromatic aldehydes, and secondary amines under neat conditions at 110 °C has been reported. The developed methodology offers various advantages, such as excellent yields (60-100%), short reaction time (5-15 min), wide substrate scope (12 examples), green reaction conditions, use of readily available catalyst, and easy purification (without column chromatography).

Synthetic molecules targeting yes associated protein activity as chemotherapeutics against cancer.

The Hippo signaling pathway extorts several signals that concomitantly target the activity of transcriptional cofactor yes associated protein (YAP). YAP is a key regulator that elicits signature gene expression by coupling with transcriptional enhanced associate domain (TEAD) family of transcriptional factors. The YAP-TEAD complex via target gene expression gets associated with the development, proliferation, and progression of cancerous cells. Moreover, YAP adorns cells with several oncogenic traits such as inhibition of apoptosis, enhanced proliferation, drug resistance, and immune response suppression, which later became associated with various diseases, particularly cancer. Therefore, inhibition of the YAP activity is an appealing and viable therapeutic target for cancer treatment. This review highlights the recent advances in existing and novel synthetic therapeutics targeting YAP inhibition and regulation. The synthetically produced YAPD93A belonging to cyclic peptides and DC-TEADin02 and vinyl sulfonamide class of compounds are the most potent compounds to inhibit the YAP-TEAD expression by targeting protein-protein interaction (IC50  = 25 nM) and palmitate binding central pocket of TEAD (IC50  = 197 nM), respectively. On the other hand, Chlorpromazine belonging to phenothiazines class has the least potential to suppress YAP via proteasomal degradation (cell viability value of <20% at 40 µM).