A novel dearomatization process to produce fused polycyclic indolines via a CF3SO3H-mediated cascade ring-opening of a β-lactam and hydroaminative cyclization is demonstrated. It provides a new strategy for the synthesis of important polycyclic indoline-2-amine derivatives in moderate to excellent yields, as well as with good functional group tolerance. Moreover, transformation of the product was performed to deliver the corresponding acid, alcohol and amide smoothly.
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http://dx.doi.org/10.1039/d1ob00712b | DOI Listing |
Inflammopharmacology
December 2024
Department of Pharmacology, Faculty of Pharmacy, The Islamia University of Bahawalpur, Bahawalpur, 63100, Punjab, Pakistan.
Juice and decoction of leaves of Suaeda fruticosa, a halophytic medicinal plant of Cholistan desert, is traditionally used to treat rheumatism. The current study was carried out to probe into in vivo anti-nociceptive, anti-inflammatory, and anti-arthritic potential of ethanolic extract of the whole plant of S. fruticosa (Et-SF) and its bioactive molecules.
View Article and Find Full Text PDFMol Divers
December 2024
Small-Molecule Drug Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai, 201203, People's Republic of China.
Overexpressed AXL kinase is involved in various human malignancies, which incurs tumor progression, poor prognosis, and drug resistance. Suppression of the aberrant AXL axis with genetic tools or small-molecule inhibitors has achieved valid antitumor efficacies in both preclinical studies and clinical antitumor campaigns. Herein we will report the design, synthesis, and structure-activity relationship (SAR) exploration of a series of anilinopyrimidine type II AXL inhibitors.
View Article and Find Full Text PDFBiol Trace Elem Res
December 2024
Department of Biochemistry, Faculty of Pharmacy, University of Sadat City (USC), Menoufia, Egypt.
Metabolic syndrome during menopause can lead to diabetes, cardiovascular problems, and increased mortality rates. Hormone replacement therapy is recommended to manage climacteric complications, but it has serious adverse effects. This study, therefore, investigated the potential of supplementing some minerals, vitamins, and natural products like boric acid, magnesium, vitamin D3, and extra virgin olive oil on metabolic status of menopausal ovariectomized rats.
View Article and Find Full Text PDFGenet Med
December 2024
Division of Genetics and Genomics, Boston Children's Hospital, Boston, MA; The Manton Center for Orphan Disease Research, Boston Children's Hospital, Boston, MA; Harvard Medical School, Boston, MA.
Purpose: Genomic sequencing of newborns (NBSeq) can initiate disease surveillance and therapy for children, and may identify at-risk relatives through reverse cascade testing. We explored genetic risk communication and reverse cascade testing among families of newborns who underwent exome sequencing and had a risk for autosomal dominant disease identified.
Methods: We conducted semi-structured interviews with parents of newborns enrolled in the BabySeq Project who had a pathogenic or likely-pathogenic (P/LP) variant associated with an autosomal dominant (AD) childhood- and/or adult-onset disease returned.
Plant Commun
December 2024
Rice Research Institute, Fujian Academy of Agricultural Sciences, Fuzhou 350019, China; State Key Laboratory of Ecological Pest Control for Fujian and Taiwan' Crops/Key Laboratory of Germplasm Innovation and Molecular Breeding of Hybrid Rice in South China/Fujian Engineering Laboratory of Crop Molecular Breeding/Fujian Key Laboratory of Rice Molecular Breeding/Fuzhou Branch, National Center of Rice Improvement of China/National Engineering Laboratory of Rice/South Base of National Key Laboratory of Hybrid Rice of China, Fuzhou 350003, China; College of Agriculture, Fujian Agriculture and Forestry University, Fuzhou 350002, China. Electronic address:
Leaf angle is a major agronomic trait that determines plant architecture, which directly affects rice planting density, photosynthetic efficiency, and yield. The plant phytohormones brassinosteroids (BRs) and the MAPK signaling cascade are known to play crucial roles in regulating the leaf angle, but the underlying molecular mechanisms are not fully understood. Here, we report a rice WRKY family transcription factor gene, OsWRKY72, which positively regulates leaf angle by affecting lamina joint development and BR signaling.
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