Formal [4 + 2] combined ionic and radical approach of vinylogous enaminonitriles to access highly substituted sulfonyl pyridazines.

Pyridazine derivatives hold significant interest due to their broad applications in pharmaceuticals and materials science, where they serve as valuable scaffolds for bioactive compounds and functional materials. Here, we report a formal [4 + 2] reaction for the synthesis of 5'-sulfonyl-4'-aryl-3-cyano substituted pyridazine compounds from the reaction between vinylogous enaminonitriles and sulfonyl hydrazides. The key features of our pyridazine synthesis include the transamidation of vinylogous enaminonitriles with sulfonyl hydrazide, radical sulfonylation of the resulting intermediate, and subsequent 6-endo-trig radical cyclization.

Advancements of anticancer agents by targeting the Hippo signalling pathway: biological activity, selectivity, docking analysis, and structure-activity relationship.

The Hippo signalling pathway is prominent and governs cell proliferation and stem cell activity, acting as a growth regulator and tumour suppressor. Defects in Hippo signalling and hyperactivation of its downstream effector's Yes-associated protein (YAP) and transcriptional co-activator with PDZ-binding motif (TAZ) play roles in cancer development, implying that pharmacological inhibition of YAP and TAZ activity could be an effective cancer treatment strategy. Conversely, YAP and TAZ can also have beneficial effects in promoting tissue repair and regeneration following damage, therefore their activation may be therapeutically effective in certain instances.

Reagent-Free Intramolecular Hydroamination of Ynone-Tethered Aryl-sulfonamide: Synthesis of Polysubstituted 4-Quinolones.

An efficient reagent-free method for the synthesis of polysubstituted 4-quinolone from 2-substituted alkynoyl aryl-sulfonamide was developed. This developed method tolerates various functional groups and gives the corresponding 4-quinolones. We have successfully extended this method to the synthesis of dihydro-4-quinolones from 2-alkenoyl aryl sulfonamide derivatives.

Poly (ADP-ribose) polymerase (PARP) inhibitors as anticancer agents: An outlook on clinical progress, synthetic strategies, biological activity, and structure-activity relationship.

Poly (ADP-ribose) polymerase (PARP) is considered an essential component in case of DNA (Deoxyribonucleic acid) damage, response by sensing DNA damage and engaging DNA repair proteins. Those proteins repair the damaged DNA via an aspect of posttranslational modification, known as poly (ADP-Ribosyl)ation (PARylation). Specifically, PARP inhibitors (PARPi) have shown better results when administered alone in a variety of cancer types with BRCA (Breast Cancer gene) mutation.

Microwave-Mediated, Catalyst-Free Synthesis of 1,2,4-Triazolo[1,5-]pyridines from Enaminonitriles.

A catalyst-free, additive-free, and eco-friendly method for synthesizing 1,2,4-triazolo[1,5-]pyridines under microwave conditions has been established. This tandem reaction involves the use of enaminonitriles and benzohydrazides, a transamidation mechanism followed by nucleophilic addition with nitrile, and subsequent condensation to yield the target compound in a short reaction time. The methodology demonstrates a broad substrate scope and good functional group tolerance, resulting in the formation of products in good-to-excellent yields.

Impact of biofertilisers on iron homeostasis and grain quality in the rice variety Uma under Elevated CO.

The diminishing nutritional quality of rice with increasing concentrations of atmospheric CO is currently a major global concern. The present study was designed with the objective of assessing the impact of biofertilisers on grain quality and iron homeostasis in rice under elevated CO. A completely randomised design with four treatments ([KAU, POP (control), POP+Azolla, POP+PGPR, and POP+AMF]), each replicated three times under ambient and elevated CO conditions, was followed.

Improved transformation of assisted by silver nanoparticles.

In transgenic plant development, the low transformation efficiency of with exogenous DNA is the major constraint, and hence, methods to improve its transformation efficiency are needed. Recently, nanoparticlemediated gene transfer has evolved as a key transformational tool in genetic transformation. Since silver nanoparticles (AgNPs) can induce pores on the cell membrane, their efficacy in the improvement of conventional calcium chloride freeze-thaw technique of transformation of was explored in this study.

Total Synthesis of Isohericerinol A and Its Analogues to Access Their Potential Neurotrophic Effects.

The secondary metabolites from are well-known to have neurotrophic and neuroprotective effects. Isohericerinol A (), isolated by our colleagues from its fruiting parts has a strong ability to increase the nerve growth factor secretion in C6 glioma cells. The current work describes the total synthesis of and its regioisomer in a few steps.

Silver nanoparticles for biolistic transformation in L.

The present study reports the use of silver nanoparticles as a gene carrier, substituting gold microcarrier for biolistic gene delivery in L Efficiency of biolistic transformation using silver nanoparticles (100 nm) was compared with that of gold microcarriers (0.6 micron) under varying helium pressure (450 psi, 650 psi, 900 psi and 1100 psi) and target distance (6 cm and 9 cm). Among the different concentrations (0.

Association mapping of drought tolerance and agronomic traits in rice (Oryza sativa L.) landraces.

Background: Asian cultivars were predominantly represented in global rice panel selected for sequencing and to identify novel alleles for drought tolerance. Diverse genetic resources adapted to Indian subcontinent were not represented much in spite harboring useful alleles that could improve agronomic traits, stress resilience and productivity. These rice accessions are valuable genetic resource in developing rice varieties suited to different rice ecosystem that experiences varying drought stress level, and at different crop stages.

High temperature induced changes in quality and yield parameters of tomato ( L.) and similarity coefficients among genotypes using SSR markers.

High temperature induced by climatic fluctuations are an important threat for plant growth, development and quality of agricultural produces. Adaptableness to environmental changes generally derives from a large set of genetic traits affecting physio-morphological, biochemical and agronomic parameters. Therefore, the identification of genotypes with higher yield and good quality parameters at high temperatures is becoming increasingly necessary for future breeding programs.

α-Hydroxy acid as an aldehyde surrogate: metal-free synthesis of pyrrolo[1,2-]quinoxalines, quinazolinones, and other N-heterocycles decarboxylative oxidative annulation reaction.

A metal-free and efficient procedure for the synthesis of pyrrolo[1,2-]quinoxalines, quinazolinones, and indolo[1,2-]quinoxaline has been developed. The key features of our method include the generation of aldehyde from α-hydroxy acid in the presence of TBHP (-butyl hydrogen peroxide), and further condensation with various amines, followed by intramolecular cyclization and subsequent oxidation to afford the corresponding quinoxalines, quinazolinones derivatives in moderate to high yields.

Morphology and Interconnected Microstructure-Driven High-Rate Capability of Li-Rich Layered Oxide Cathodes.

A Li-rich layered oxide (LLO) cathode with morphology-dependent electrochemical performance with the composition LiMnNiCoO in three different microstructural forms, namely, randomly shaped particles, platelets, and nanofibers, is synthesized through the solid-state reaction (SSR-LLO), hydrothermal method (HT-LLO), and electrospinning process (ES-LLO), respectively. Even though the cathodes possess different morphologies, structurally they are identical. The elemental dispersion studies using energy-dispersive X-ray spectroscopy mapping in scanning transmission electron microscopy show uniform distribution of elements.

Water stress mediated root trait dynamics and identification of microsatellite markers associated with root traits in rice ( L.).

To identify microsatellite markers associated with root traits for drought tolerance in rice ( L.) a study was conducted at Department of Plant Physiology, College of Agriculture, Trivandrum, Kerala Agricultural University. A set of thirty-five rice genotypes were exposed to water stress and evaluated for physio-morphological components as indices of water stress tolerance.

Aza-BODIPY nanomicelles as versatile agents for the in vitro and in vivo singlet oxygen-triggered apoptosis of human breast cancer cells.

Herein, we synthesised four aza-BODIPY dyes (1-4) with the singlet oxygen generation quantum yield values of ca. 65-85%. Furthermore, we formulated a nanomedicine by encapsulating these dyes into an amphiphilic micelle, DSPE.

Hematite/M (M = Au, Pd) Catalysts Derived from a Double-Hollow Prussian Blue Microstructure: Simultaneous Catalytic Reduction of - and -Nitrophenols.

Present study deals with hematite/M (M = Au, Pd) catalysts converted from a double-hollow Prussian blue microstructure (DHPM). The unique Prussian blue (PB) microstructure (MS) is prepared by a template-free solvothermal synthetic route in a single-step reaction. An amine-functionalized silicate sol-gel matrix (SSG) has served as the structure-directing agent cum stabilizer for making DHPM.

Variations in implementation of bladder training for overactive bladder: an online international survey.

We distributed an online questionnaire to 365 health care professionals specialising in urogynaecology, using the International Urogynaecology Association (IUGA) and British Society of Urogynecolgoy (BSUG) directories to investigate how the bladder training (BT) is provided in their units. We assessed the techniques provided, who provides them, and how these techniques are implemented and taught to the patients. Two hundred and thirteen (59%) completed responses have been received.

Transition metal-free synthesis of quinazolinones using dimethyl sulfoxide as a synthon.

Biologically important quinazolinones have been synthesized from 2-aminobenzamides and DMSO. The key feature of the reaction is the utilization of DMSO as a methine source for intramolecular oxidative annulation. The CNS depressant drug methaqualone has also been synthesized by our methodology.

A novel approach for increasing transformation efficiency in DH5α cells using silver nanoparticles.

The present study is the first report on the application of silver nanoparticles for efficient bacterial transformation. EC50 value of 100 nm silver nanoparticles against DH5α cells was recorded as 4.49 mg L in toxicity assay.

Calcium alginate encapsulated synthetic seed production in L. for germplasm exchange and distribution.

L. (Plumbaginaceae), is a medicinal shrub commercially exploited for its naphthoquinone principle, plumbagin, extracted from the roots especially for treating skin disorders. As the plant is exploited from the wild without being replenished, conservation of the species becomes inevitable.

In Vitro and In Vivo Demonstration of Human-Ovarian-Cancer Necrosis through a Water-Soluble and Near-Infrared-Absorbing Chlorin.

With the objective of developing efficient sensitizers for therapeutic applications, we synthesized a water-soluble 5,10,15,20-tetrakis(3,4-dihydroxyphenyl)chlorin (TDC) and investigated its in vitro and in vivo biological efficacy, comparing it with the commercially available sensitizers. TDC showed high water solubility (6-fold) when compared with that of Foscan and exhibited excellent triplet-excited-state (84%) and singlet-oxygen (80%) yields. In vitro photobiological investigations in human-ovarian-cancer cell lines SKOV-3 showed high photocytotoxicity, negligible dark toxicity, rapid cellular uptake, and specific localization of TDC in neoplastic cells as assessed by flow-cytometric cell-cycle and propidium iodide staining analysis.

Synthesis, biological evaluation, and metabolic stability of chlorogenic acid derivatives possessing thiazole as potent inhibitors of α-MSH-stimulated melanogenesis.

A series of catechol and dioxolane analogs containing thiazole CGA derivatives have been synthesized and evaluated for their inhibitory activity against α-MSH. The inhibitory activity was improved by replacing an α,β-unsaturated carbonyl of previously reported caffeamides with thiazole motif. Surprisingly, compound 7d, one of the derivatives of dioxolane analogs, displayed the most potent inhibitory activity with an IC of 0.

Synthesis and biological evaluation of caffeic acid derivatives as potent inhibitors of α-MSH-stimulated melanogenesis.

We have disclosed our effort to develop caffeic acid derivatives as potent and non-toxic inhibitors of α-MSH-stimulated melanogenesis to treat pigmentation disorders and skin medication including a cosmetic skin-whitening agent. The SAR studies revealed that cyclohexyl ester and secondary amide derivatives of caffeic acid showed significant inhibitory activities.

A microdroplet cell culture based high frequency somatic embryogenesis system for pigeonpea, Cajanus cajan (L.) Millsp.

A protocol for high frequency production of somatic embryos was worked out in pigeonpea, Cajanus cajan (L.) Millsp. The protocol involved sequential employment of embryogenic callus cultures, low density cell suspension cultures and a novel microdroplet cell culture system.