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Keywords = SPLAM

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13 pages, 2101 KB  
Article
Design and Synthesis of E7820/Tasisulam Hybrids as Potential DCAF15 Binders
by Sofiane Hocine, Victor Cosson, Remi Calandrino, Timea Baló, Jayson Alves Bordelo, Sébastien Triboulet, Laure Caruana, Laurence Klipfel, Sandrine Calis, András Herner and Stephen Hanessian
Reactions 2025, 6(2), 34; https://doi.org/10.3390/reactions6020034 - 20 May 2025
Viewed by 2358
Abstract
We describe the design and synthesis of a series of N-[arylsulfonyl]-1H-pyrrole-2-carboxamides as hybrid analogs of the DCAF15 binders E7820 and tasisulam, two representative SPLAMs (sulfonamide-containing molecular glues). These hybrid molecules were designed to combine the key interactions of both parent ligands within the [...] Read more.
We describe the design and synthesis of a series of N-[arylsulfonyl]-1H-pyrrole-2-carboxamides as hybrid analogs of the DCAF15 binders E7820 and tasisulam, two representative SPLAMs (sulfonamide-containing molecular glues). These hybrid molecules were designed to combine the key interactions of both parent ligands within the DCAF15 binding site, as supported by docking studies. Binding affinity was evaluated using fluorescence polarization assays, and structure–activity relationships were established, highlighting the importance of dichlorinated pyrrole moieties. Selected compounds were also tested in HCT116 cells to assess in vitro activity. Full article
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22 pages, 2652 KB  
Article
Design and Synthesis of 7-(N-Aryl Pyrrolidinyl) Indoles as Potential DCAF15 Binders
by Ravi Devarajappa, Scarlett Kiyeleko, Sofiane Hocine, Victor Cosson, Remi Calandrino, Timea Baló, Jayson Alves Bordelo, Sébastien Triboulet, Laure Caruana, Laurence Klipfel, Sandrine Calis, András Herner and Stephen Hanessian
Reactions 2025, 6(1), 20; https://doi.org/10.3390/reactions6010020 - 7 Mar 2025
Cited by 1 | Viewed by 2459
Abstract
We describe the design and synthesis of a series of 7-(N-aryl pyrrolidinyl) indoles and oxo-analogs as isosteric mimics of the DCAF15 binder E7820, a well-known member of aryl sulfonamides known as SPLAMs. The functionalization of C-7 in indoles was achieved by metal-catalyzed CH-activation [...] Read more.
We describe the design and synthesis of a series of 7-(N-aryl pyrrolidinyl) indoles and oxo-analogs as isosteric mimics of the DCAF15 binder E7820, a well-known member of aryl sulfonamides known as SPLAMs. The functionalization of C-7 in indoles was achieved by metal-catalyzed CH-activation with unexpected results. Binding assays revealed the pyrrolidine N-aryl carboxylic acid analog to be as equally active as E7820. Full article
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26 pages, 7458 KB  
Review
A Comprehensive Study of Mobile Robot: History, Developments, Applications, and Future Research Perspectives
by Ravi Raj and Andrzej Kos
Appl. Sci. 2022, 12(14), 6951; https://doi.org/10.3390/app12146951 - 8 Jul 2022
Cited by 138 | Viewed by 22818
Abstract
Intelligent mobile robots that can move independently were laid out in the real world around 100 years ago during the second world war after advancements in computer science. Since then, mobile robot research has transformed robotics and information engineering. For example, robots were [...] Read more.
Intelligent mobile robots that can move independently were laid out in the real world around 100 years ago during the second world war after advancements in computer science. Since then, mobile robot research has transformed robotics and information engineering. For example, robots were crucial in military applications, especially in teleoperations, when they emerged during the second world war era. Furthermore, after the implementation of artificial intelligence (AI) in robotics, they became autonomous or more intelligent. Currently, mobile robots have been implemented in many applications like defense, security, freight, pattern recognition, medical treatment, mail delivery, infrastructure inspection and developments, passenger travel, and many more because they are more intelligent nowadays with artificial intelligence technology. To study the developments of mobile robots, we have studied an extensive literature survey of the last 50 years. In this article, we discuss a complete century of mobile robotics research, major sensors used in robotics, some major applications of mobile robots, and their impact on our lives and in applied engineering. Full article
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