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View article: Thiazole substitution of a labile amide bond—a new option toward antiplasmodial pantothenamide-mimics
Thiazole substitution of a labile amide bond—a new option toward antiplasmodial pantothenamide-mimics Open
The emergence and spread of artemisinin-partial resistant, malaria-causing Plasmodium falciparum provide the impetus for developing novel antimalarials. Pantothenamides are potent inhibitors of malaria parasite proliferation; however, thei…
View article: Thiazole substitution of a labile amide bond - a new option towards stable pantothenamide-mimics
Thiazole substitution of a labile amide bond - a new option towards stable pantothenamide-mimics Open
The emergence and spread of artemisinin-resistant, malaria-causing P. falciparum provide the impetus for the development of novel antimalarials. Pantothenamides are potent inhibitors of malaria parasite proliferation, however their clinica…
View article: Organic Transformations Utilizing 1,5,7‐Triazabicyclo[4.4.0]Dec‐5‐Ene (TBD): A Tale of Two Nitrogens
Organic Transformations Utilizing 1,5,7‐Triazabicyclo[4.4.0]Dec‐5‐Ene (TBD): A Tale of Two Nitrogens Open
1,5,7‐Triazabicyclo[4.4.0]dec‐5‐ene (TBD) is a bicyclic guanidine with booming applications. Bearing both a sp 2 ‐hybridized nitrogen and an adjacent N−H bond, TBD is a multifunctional and versatile reagent that is able to promote a variet…
View article: 1,5,7‐Triazabicyclo[4.4.0]dec‐5‐ene (TBD): An Organocatalyst for Rapid Access to 3‐Hydroxyisoindolin‐1‐ones
1,5,7‐Triazabicyclo[4.4.0]dec‐5‐ene (TBD): An Organocatalyst for Rapid Access to 3‐Hydroxyisoindolin‐1‐ones Open
The readily available organocatalyst 1,5,7‐triazabicyclo[4.4.0]dec‐5‐ene (TBD) was used for the rapid synthesis of 3‐hydroxyisoindolin‐1‐ones from 3‐alkylidenephthalides. The transformation occurs at room temperature and requires less solv…
View article: Conversion of Aldehydes to Branched or Linear Ketones via Regiodivergent Rhodium-Catalyzed Vinyl Bromide Reductive Coupling–Redox Isomerization Mediated by Formate
Conversion of Aldehydes to Branched or Linear Ketones via Regiodivergent Rhodium-Catalyzed Vinyl Bromide Reductive Coupling–Redox Isomerization Mediated by Formate Open
A regiodivergent catalytic method for direct conversion of aldehydes to branched or linear alkyl ketones is described. Rhodium complexes modified by P tBu2Me catalyze formate-mediated aldehyde-vinyl bromide reductive coupling-redox isomeri…
View article: Therapeutic inhibition of SGK1 suppresses colorectal cancer
Therapeutic inhibition of SGK1 suppresses colorectal cancer Open
Colorectal cancer (CRC) is one of the leading causes of death worldwide. Thus, the development of new therapeutic targets for CRC treatment is urgently needed. SGK1 is involved in various cellular activities, and its dysregulation can resu…
View article: Development of a new analog of SGK1 inhibitor and its evaluation as a therapeutic molecule of colorectal cancer
Development of a new analog of SGK1 inhibitor and its evaluation as a therapeutic molecule of colorectal cancer Open
Colorectal cancer (CRC) is one of the most leading causes of cancer-related death worldwide. The serum and glucocorticoid inducible kinase SGK1 is highly expressed and involved in several tumors. GSK650394, a SGK1 inhibitor, has been prove…