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Privileged Scaffold Hybridization in the Design of Carbonic Anhydrase Inhibitors.
Molecules
September 2024
Department of Life and Environmental Sciences, University of Cagliari, Cittadella Universitaria di Monserrato, Monserrato, 09042 Cagliari, Italy.
Human Carbonic Anhydrases (hCA) are enzymes that contribute to cancer's development and progression. Isoforms IX and XII have been identified as potential anticancer targets, and, more specifically, hCA IX is overexpressed in hypoxic tumor cells, where it plays an important role in reprogramming the metabolism. With the aim to find new inhibitors towards IX and XII isoforms, the hybridization of the privileged scaffolds isatin, dihydrothiazole, and benzenesulfonamide was investigated in order to explore how it may affect the activity and selectivity of the hCA isoforms.
View Article and Find Full Text PDFSynthesis, Fluorescence, and Bioactivity of Novel Isatin Derivatives.
J Phys Chem B
June 2024
School of Life Sciences and Health Engineering, Jiangnan University, Jiangsu 214122, China.
Article Synopsis
- - The isatin group, known for its significance in drug discovery, was utilized to create new SHP1 inhibitors with fluorescent features for research purposes.
- - A newly synthesized compound demonstrated strong inhibition of SHP1 activity (IC of 11 ± 3 μM) and effectively reduced cell proliferation in MV-4-11 cells by 92% at 20 μM concentration.
- - The compound exhibited favorable fluorescent characteristics and low toxicity, allowing for blue fluorescent imaging in HeLa cells, which can advance our understanding of SHP1 in biological contexts and therapeutic applications.
Electrochemical and photochemical reaction of isatins: a decade update.
Org Biomol Chem
May 2024
Department of Chemistry, St Joseph's University, 36 Lalbagh Road, Shanthinagar, Bengaluru-560027, Karnataka, India.
This review presents the latest progress in photochemical and electrochemical reactions involving isatins. Isatin and its functionalized scaffolds , oxindoles, spirooxindoles, and quinolines are privileged heterocycles as they are largely present in several agrochemical, natural products, and pharmaceuticals. Thus, the functionalization of isatins using sustainable approaches, , electro- and photochemical methods is of recent research interest worldwide.
View Article and Find Full Text PDFDesign and synthesis of benzo[b]thiophene-based hybrids as novel antitubercular agents against MDR/XDR Mycobacterium tuberculosis.
Arch Pharm (Weinheim)
February 2024
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Kafrelsheikh University, Kafrelsheikh, Egypt.
In an effort to support the global fight against tuberculosis (TB), which is widely recognized as the most lethal infectious disease worldwide, we present the design and synthesis of new benzo[b]thiophene-based hybrids as promising candidates for the management of multidrug-resistant (MDR)/extensively drug-resistant (XDR) Mycobacterium tuberculosis. The isatin motif was incorporated into the target hybrids as it represents a privileged scaffold in antitubercular drug discovery. Since lipophilicity plays a pivotal role in the anti-TB agents' activity, the lipophilicity of the target hybrids was manipulated via the development of two series of N-1 methyl and N-1 benzyl substituted isatins (6a-h and 9a-h, respectively).
View Article and Find Full Text PDFRecent progress in the synthesis of natural product inspired bioactive glycohybrids.
Carbohydr Res
December 2023
Glycochemistry Laboratory, School of Physical Sciences, Jawaharlal Nehru University, New Delhi, 110067, India. Electronic address:
Carbohydrates are a basic structural component that are indispensable to all cellular processes. In addition to being employed as chiral starting materials in the synthesis of a variety of natural products, carbohydrates are recognized as naturally occurring molecules having an enormous variety of functional, stereochemical, and structural properties. The understanding and biological roles of carbohydrate derived molecules can be greatly improved by selectively synthesizing functional carbohydrates through incorporating them with privileged scaffolds.
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