Design and discovery of carboxamide-based pyrazole conjugates with multifaceted potential against Triple-Negative Breast cancer MDA-MB-231 cells.

We report the design, synthesis, and validation of carboxamide-based pyrazole and isoxazole conjugates with a multifaceted activity against Breast Cancer Cell Line MDA-MB-231. The study established that amongst the series, N-(3,5-bis(trifluoromethyl)benzyl)-3-(3,4,5-trimethoxyphenyl)-1H-pyrazole-5-carboxamide (5g) exhibits the highest potency in inhibiting Breast Cancer Cell Line MDA-MB-231 with an IC value of 15.08 ± 0.

Impact of bioclimatic factors on physio-biochemical and molecular response of slow-growing poultry reared in tropics.

Most of the climatic studies projected on heat stress have considered heat extremes, but not the humidity. Hence, this work was carried out to evaluate thermotolerance, production performance, physio-biochemical and immunological response of slow-growing poultry towards various temperature-humidity levels in coastal climate. A total of 240 straight run CARI-Debendra birds were reared in three groups based on temperature-humidity indices (THI > 80, = 75-80 and < 75).

Marine Based Natural Products: Exploring the Recent Developments in the Identification of Antimicrobial Agents.

The marine ecosystem is the less explored, biologically diverse, and vastest resource to discover novel antimicrobial agents. In recent decades' antimicrobial drugs are losing their effectiveness due to the growing resistance among pathogens, which causes diseases to have considerable death rates across the globe. Therefore, there is a need for the discovery of new antibacterials that can reach the market.

Correction: I/TBHP mediated diastereoselective synthesis of spiroaziridines.

Correction for 'I/TBHP mediated diastereoselective synthesis of spiroaziridines' by Kizhakkan Thiruthi Ashitha , , 2020, , 1588-1593, DOI: 10.1039/C9OB02711D.

I/TBHP mediated diastereoselective synthesis of spiroaziridines.

Eventhough spiroheterocycles are considered as emerging drug candidates, synthesis of spiroaziridines has not been well explored so far. Herein, we disclose an efficient I2/TBHP mediated diastereoselective synthesis of N-alkyl spiroaziridines from primary amines and easily accessible α,β-unsaturated ketones. The reaction is also compatible for the synthesis of 2-aroylaziridines.

Synthesis of symmetrical and unsymmetrical triarylpyrylium ions via an inverse electron demand Diels-Alder reaction.

BF·OEt mediated inverse electron demand Diels-Alder (IEDDA) reaction of chalcones with aryl acetylenes is reported for the synthesis of symmetrical and unsymmetrical 2,4,6-triarylpyrylium ions. The protocol provides an effective one-pot method for the utilization of readily available simple substrates under mild reaction conditions leading to a diverse array of pyrylium ions in moderately good yield.

Discovery of Natural Product Derived Labdane Appended Triazoles as Potent Pancreatic Lipase Inhibitors.

Obesity contributes to the genesis of many metabolic disorders including dyslipidemia, coronary heart disease (CHD), nonalcoholic fatty liver, type 2 diabetes, etc. Pancreatic lipase plays a vital role in food fat digestion and absorption. Therefore, to control obesity, inhibition of pancreatic lipase is the active therapy.

BF·OEt-Mediated Tandem Annulation: A Strategy To Construct Functionalized Chromeno- and Pyrano-Fused Pyridines.

A simple and efficient one-pot annulation of arylidenones, alkynes, and nitriles in the presence of BF·OEt is described. A highly functionalized variety of N-substituted pyridine-fused chromeno and pyrano derivatives were obtained with satisfactory yields under mild reaction conditions. The method was proven to be valid for the synthesis of a diverse library of chromeno[3,4-c]pyridines, thiochromeno[3,4-c]pyridines, pyrano[3,4-c]pyridines, and thiopyrano[3,4-c]pyridine derivatives from readily accessible substrates.

BF·EtO mediated one-step synthesis of N-substituted-1,2-dihydropyridines, indenopyridines and 5,6-dihydroisoquinolines.

A simple and efficient one-pot synthesis of N-substituted-1,2-dihydropyridines, indenopyridines and 5,6-dihydroisoquinolines by a BF·EtO mediated novel methodology, from easily available α,β-unsaturated ketones/arylidene ketones, phenyl acetylenes and substituted nitriles, has been described. This novel annulation provides quick access to complex polycyclic frameworks with an excellent substrate scope.