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An efficient redox-neutral palladium-catalyzed system has been developed to introduce indole and pyrrole units to a wide range of bioactive molecules late-stage aryl C-H activation, providing a robust tool for medicinal chemists to explore structure-activity relationships (SARs). Furthermore, the successful gram-scale reaction and subsequent synthetic investigations demonstrate the potential application of this established method in organic synthesis, materials science, and biochemistry.
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http://dx.doi.org/10.1039/d4cc04528a | DOI Listing |
ACS Infect Dis
September 2025
Department of Biochemistry, University of Texas Southwestern Medical Center, Dallas, Texas 75390, United States.
Malaria treatments are compromised by drug resistance, creating an urgent need to discover new drugs. We used a phenotypic high-throughput screening (HTS) platform to identify new antimalarials, uncovering three related pyrrole-, indole-, and indoline-based series with a shared α-azacyclic acetamide core. These compounds showed fast-killing activity on asexual blood-stage parasites, were not cytotoxic, and disrupted parasite intracellular pH and Na regulation similarly to cipargamin (KAE609), a clinically advanced inhibitor of the Na pump (ATP4).
View Article and Find Full Text PDFCroat Med J
August 2025
Mehrdad Payandeh, Internal Medicine Department, School of Medicine, Kermanshah University of Medical Sciences, Beheshti Blvd, 83VX+PCM, Kermanshah, Iran,
Locally advanced renal cell carcinoma (RCC) presents significant therapeutic challenges, particularly in resource-limited settings with restricted access to new therapies. This report describes a new exploratory multimodal therapeutic approach for a patient with locally advanced clear cell RCC (ccRCC) with adrenal and lymph node metastases. A 45-year-old woman presented with an incidentally discovered 9-cm mass in the left kidney, which was later diagnosed as grade-2 ccRCC with adrenal and lymph node involvement.
View Article and Find Full Text PDFPhysiol Plant
September 2025
College of Natural Resource and Environment, Northwest A&F University, Yangling, Shaanxi, China.
Nitrogen (N) is essential for plant growth, but excessive fertilizer use decreases nitrogen use efficiency (NUE) and raises environmental concerns. This study investigated the effect of exogenous abscisic acid (ABA; 50 μM) application on rapeseed (Brassica napus L.) plants under hydroponic conditions with high (7.
View Article and Find Full Text PDFLancet Oncol
September 2025
Key Laboratory of Carcinogenesis and Translational Research (Ministry of Education/Beijing), Department of Genitourinary Oncology, Peking University Cancer Hospital & Institute, Beijing, China. Electronic address:
Background: The underexplored potential of PD-L1 blockade in advanced renal cell carcinoma highlights an urgent need for novel agents. This trial aimed to compare benmelstobart (a novel PD-L1 inhibitor) plus anlotinib with sunitinib as first-line treatment for advanced renal cell carcinoma.
Methods: ETER100 was a multicentre, randomised, open-label, phase 3 trial conducted at 37 medical sites in China.
RSC Adv
August 2025
Department of Chemistry, National Institute of Technology Karnataka Surathkal-575025 India
Azobenzenes (Ph-N[double bond, length as m-dash]N-Ph) are well-known photochromic compounds with widespread applications. Replacing one or both phenyl rings of azobenzenes with heteroarenes leads to a new class of compounds known as azoheteroarenes (Het-N[double bond, length as m-dash]N-Ph/Het). Azoheteroarenes have gained attention as promising alternatives to traditional azobenzenes in the field of photopharmacology due to their ability to undergo photoswitching under visible light.
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