Sun.May 25, 2025

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Design, synthesis and biological evaluation of the activity-based probes for FGFR covalent inhibitor

Covalent Modifiers

Dandan Zhu, Zijian Zheng, Huixin Huang, Xiaojuan Chen, Shuhong Zhang, Zhuchu Chen, Ting Liu, Guangyu Xu, Ying Fu, Yongheng Chen, European Journal of Medicinal Chemistry , 2025 [link] Fibroblast growth factor receptors (FGFRs) represent promising therapeutic targets in various malignancies, yet the clinical application of FGFR covalent inhibitors has been impeded by several significant challenges, including unquantifiable target engagement, undefined off-target effects, and the emergence of drug

Drugs 173
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Quieter Classrooms May Help Calm Kids, Study Shows

Drugs.com

SUNDAY, May 25, 2025 The first day of preschool can be tough lots of new faces, unfamiliar sounds and the sudden goodbye to Mom or Dad can be overwhelming. But what if something as simple as the ceiling could make it a little easier?New res.

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Design, Synthesis and Biological Evaluation of POLRMT Inhibitors for the Treatment of Acute Myeloid Leukemia

Chemical Biology and Drug Design

Based on the previously reported crystal structure of the POLRMT inhibitor IMT1B, a series of derivatives with additional hydrophobic occupancy groups were designed and synthesized using a scaffold jumping strategy. A new potent POLRMT inhibitor ( 10a ) showed potent antiproliferative activity in MOLM-13 cells that disrupted mitochondrial function and induced apoptosis.

Treatment 100
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Synthesis of Novel Thiazole/Thiadiazole Conjugates of Fluoroquinolones as Potent Antibacterial and Antimycobacterial Agents

Chemical Biology and Drug Design

Twenty new fluoroquinolone-azole conjugates were synthesized. The synthesized compounds were screened vs. various bacterial and mycobacterial strains. Most of the compounds showed potent antibacterial activity. Compound 35 was equipotent with ciprofloxacin vs. M. tuberculosis H37Rv. In silico and invitro study of compound 35 against DNA-gyrase enzyme were performed.

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Bridging Innovation & Patient Care: The Growing Role of AI

Speaker: Simran Kaur, Co-founder & CEO at Tattva.Health

AI is transforming clinical trials—accelerating drug discovery, optimizing patient recruitment, and improving data analysis. But its impact goes far beyond research. As AI-driven innovation reshapes the clinical trial process, it’s also influencing broader healthcare trends, from personalized medicine to patient outcomes. Join this new webinar featuring Simran Kaur for an insightful discussion on what all of this means for the future of healthcare!