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Article ; Online: A novel procedure for the synthesis of borylated quinolines and its application in the development of potential boron-based homeodomain interacting protein kinase 2 (HIPK2) inhibitors.

Das, Bhaskar C / Yadav, Pratik / Das, Sasmita / He, John Cijiang

RSC advances

2022 Volume 12, Issue 37, Page(s) 24187–24191

Abstract: Herein, we demonstrate a Pd catalyzed C-4 borylation of structurally complex chloroquinolines with bis(pinacolato)diboron under relatively simple and efficient conditions. Moreover, the borylated quinolines were converted into oxaborole, trifluoroborate ... ...

Abstract	Herein, we demonstrate a Pd catalyzed C-4 borylation of structurally complex chloroquinolines with bis(pinacolato)diboron under relatively simple and efficient conditions. Moreover, the borylated quinolines were converted into oxaborole, trifluoroborate salt and boronic acid and also rendered in the Suzuki reaction successfully. The method was also applied for the synthesis of potential boron-based homeodomain interacting protein kinase 2 (HIPK2) inhibitors. The strategy opens up new avenues for the functionalization of quinolines as potential probes and pharmacological agents for future biomedical research.
Language	English
Publishing date	2022-08-25
Publishing country	England
Document type	Journal Article
ISSN	2046-2069
ISSN (online)	2046-2069
DOI	10.1039/d2ra05063c
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Article ; Online: Stimuli-Responsive Boron-Based Materials in Drug Delivery.

Das, Bhaskar C / Chokkalingam, Parthiban / Masilamani, Pavithra / Shukla, Srushti / Das, Sasmita

International journal of molecular sciences

2023 Volume 24, Issue 3

Abstract: Drug delivery systems, which use components at the nanoscale level as diagnostic tools or to release therapeutic drugs to particular target areas in a regulated manner, are a fast-evolving field of science. The active pharmaceutical substance can be ... ...

Abstract	Drug delivery systems, which use components at the nanoscale level as diagnostic tools or to release therapeutic drugs to particular target areas in a regulated manner, are a fast-evolving field of science. The active pharmaceutical substance can be released via the drug delivery system to produce the desired therapeutic effect. The poor bioavailability and irregular plasma drug levels of conventional drug delivery systems (tablets, capsules, syrups, etc.) prevent them from achieving sustained delivery. The entire therapy process may be ineffective without a reliable delivery system. To achieve optimal safety and effectiveness, the drug must also be administered at a precision-controlled rate and the targeted spot. The issues with traditional drug delivery are overcome by the development of stimuli-responsive controlled drug release. Over the past decades, regulated drug delivery has evolved considerably, progressing from large- and nanoscale to smart-controlled drug delivery for several diseases. The current review provides an updated overview of recent developments in the field of stimuli-responsive boron-based materials in drug delivery for various diseases. Boron-containing compounds such as boron nitride, boronic acid, and boron dipyrromethene have been developed as a moving field of research in drug delivery. Due to their ability to achieve precise control over drug release through the response to particular stimuli (pH, light, glutathione, glucose or temperature), stimuli-responsive nanoscale drug delivery systems are attracting a lot of attention. The potential of developing their capabilities to a wide range of nanoscale systems, such as nanoparticles, nanosheets/nanospheres, nanotubes, nanocarriers, microneedles, nanocapsules, hydrogel, nanoassembly, etc., is also addressed and examined. This review also provides overall design principles to include stimuli-responsive boron nanomaterial-based drug delivery systems, which might inspire new concepts and applications.
MeSH term(s)	Boron ; Stimuli Responsive Polymers ; Drug Delivery Systems ; Nanoparticles/chemistry ; Nanospheres ; Nanocapsules ; Drug Carriers/chemistry ; Drug Liberation
Chemical Substances	Boron (N9E3X5056Q) ; Stimuli Responsive Polymers ; Nanocapsules ; Drug Carriers
Language	English
Publishing date	2023-02-01
Publishing country	Switzerland
Document type	Journal Article ; Review
ZDB-ID	2019364-6
ISSN	1422-0067 ; 1422-0067 ; 1661-6596
ISSN (online)	1422-0067
ISSN	1422-0067 ; 1661-6596
DOI	10.3390/ijms24032757
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Article ; Online: Development of a New Methodology for Dearomative Borylation of Coumarins and Chromenes and Its Applications to Synthesize Boron-Containing Retinoids.

Das, Bhaskar C / Yadav, Pratik / Das, Sasmita / Saito, Mariko / Evans, Todd

Molecules (Basel, Switzerland)

2023 Volume 28, Issue 3

Abstract: Dearomative borylation of coumarins and chromenes via conjugate addition represents a relatively unexplored and challenging task. To address this issue, herein, we report a new and general copper (I) catalyzed dearomative borylation process to synthesize ...

Abstract	Dearomative borylation of coumarins and chromenes via conjugate addition represents a relatively unexplored and challenging task. To address this issue, herein, we report a new and general copper (I) catalyzed dearomative borylation process to synthesize boron-containing oxacycles. In this report, the borylation of coumarins, chromones, and chromenes comprising functional groups, such as esters, nitriles, carbonyls, and amides, has been achieved. In addition, the method generates different classes of potential boron-based retinoids, including the ones with oxadiazole and anthocyanin motifs. The borylated oxacycles can serve as suitable intermediates to generate a library of compounds.
MeSH term(s)	Benzopyrans ; Boron ; Coumarins ; Copper ; Amides
Chemical Substances	Benzopyrans ; Boron (N9E3X5056Q) ; Coumarins ; Copper (789U1901C5) ; Amides
Language	English
Publishing date	2023-01-20
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	1413402-0
ISSN	1420-3049 ; 1431-5165 ; 1420-3049
ISSN (online)	1420-3049
ISSN	1431-5165 ; 1420-3049
DOI	10.3390/molecules28031052
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Article: A novel procedure for the synthesis of borylated quinolines and its application in the development of potential boron-based homeodomain interacting protein kinase 2 (HIPK2) inhibitors

Das, Bhaskar C. / Yadav, Pratik / Das, Sasmita / He, John Cijiang

RSC advances. 2022 Aug. 25, v. 12, no. 37

2022

Abstract	Herein, we demonstrate a Pd catalyzed C-4 borylation of structurally complex chloroquinolines with bis(pinacolato)diboron under relatively simple and efficient conditions. Moreover, the borylated quinolines were converted into oxaborole, trifluoroborate salt and boronic acid and also rendered in the Suzuki reaction successfully. The method was also applied for the synthesis of potential boron-based homeodomain interacting protein kinase 2 (HIPK2) inhibitors. The strategy opens up new avenues for the functionalization of quinolines as potential probes and pharmacological agents for future biomedical research.
Keywords	Suzuki reaction ; biomedical research ; boronic acids ; protein kinases ; quinolines
Language	English
Dates of publication	2022-0825
Size	p. 24187-24191.
Publishing place	The Royal Society of Chemistry
Document type	Article
ISSN	2046-2069
DOI	10.1039/d2ra05063c
Database	NAL-Catalogue (AGRICOLA)

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Article: Synthesis of a boron-containing amidoxime reagent and its application to synthesize functionalized oxadiazole and quinazolinone derivatives

Das, Bhaskar C. / Nandwana, Nitesh K. / P.Ojha, Devi / Das, Sasmita / Evans, Todd

Tetrahedron letters. 2022 Mar. 02, v. 92

2022

Abstract: Herein, we report the design, synthesis and application of a borylated amidoxime reagent for the direct synthesis of functionalized oxadiazole and quinazolinone derivatives. This reagent exhibits broad synthetic utility to obtain a variety of ... ...

Abstract	Herein, we report the design, synthesis and application of a borylated amidoxime reagent for the direct synthesis of functionalized oxadiazole and quinazolinone derivatives. This reagent exhibits broad synthetic utility to obtain a variety of biologically relevant drug-like molecules. It can be easily prepared at large scale from relatively inexpensive reagents, and can undergo facile transformations to obtain target compounds. The developed amidoxime reagent was synthesized from 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile and hydroxyl amine hydrochloride using N,N-diisopropylethylamine as a base in ethanol under reflux conditions. Overall advantages include a metal-free route to boronated oxadiazoles, quinazolinone derivatives, and restriction of the multistep sequences. Importantly, the boron-rich pharmacophore derived compounds were obtained through an efficient and inexpensive strategy.
Keywords	ethanol ; oxadiazoles ; pharmacology
Language	English
Dates of publication	2022-0302
Publishing place	Elsevier Ltd
Document type	Article
ZDB-ID	204287-3
ISSN	1873-3581 ; 0040-4039
ISSN (online)	1873-3581
ISSN	0040-4039
DOI	10.1016/j.tetlet.2022.153657
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Zs.A 2837: Show issues

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Article ; Online: Microbial communities modulating brain functioning and behaviors in zebrafish: A mechanistic approach.

Mohanta, Larica / Das, Bhaskar C / Patri, Manorama

Microbial pathogenesis

2020 Volume 145, Page(s) 104251

Abstract: Microbiota plays a vital role in maintaining their host's physiology, development, reproduction, immune system, nutrient metabolism, brain chemistry and its behavior. How the gut microbiota modulates the brain function altering cognitive and fundamental ... ...

Abstract	Microbiota plays a vital role in maintaining their host's physiology, development, reproduction, immune system, nutrient metabolism, brain chemistry and its behavior. How the gut microbiota modulates the brain function altering cognitive and fundamental behavior patterns related to specific functional changes is unclear. Recent studies provide holistic approaches which show gut microbiota can greatly sway all aspects of physiology including gut-brain communication, brain function and behavior by establishing a bi-directional link between the gut and brain. Among these studies, to our knowledge, the present review focus on the new mechanistic basis that relates the microbiota of the intestine with diseases of the nervous system causing behavioral alteration in zebrafish (Danio rerio) during development. The current review on microbiota-gut-brain axis communication showed a high instability of the microbiome at early stage of development in zebrafish. Probiotics restore the composition of the gut microbiota by producing neuroactive compounds and introduce beneficial functions to gut microbial communities, resulting in amelioration of gut inflammation and other intestinal disease phenotypes. Therefore, the present review mainly highlights the mechanistic way of gut-brain function, including neuronal, hormonal, immunological signaling with production of bacterial metabolites. This study consider current knowledge that may enable us to increase our understanding to know how the gut microbiota establishes a connection with brain modulating the gut-brain signaling by alteration of the neurochemistry such as GABA and serotonin levels in brain to control host behavior. Further studies are needed to define the exact microbial and host mechanism in GI disease states and functional syndromes.
MeSH term(s)	Animals ; Brain ; Gastrointestinal Microbiome ; Microbiota ; Probiotics ; Zebrafish
Language	English
Publishing date	2020-05-11
Publishing country	England
Document type	Journal Article ; Review
ZDB-ID	632772-2
ISSN	1096-1208 ; 0882-4010
ISSN (online)	1096-1208
ISSN	0882-4010
DOI	10.1016/j.micpath.2020.104251
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Article: Magmas Inhibition in Prostate Cancer: A Novel Target for Treatment-Resistant Disease.

Yang, Jianhui / Das, Bhaskar C / Aljitawi, Omar / Kumar, Avinash / Das, Sasmita / Van Veldhuizen, Peter

Cancers

2022 Volume 14, Issue 11

Abstract: The purpose of our study was to evaluate Magmas as a potential target in prostate cancer. In addition, we evaluated our synthetic Magmas inhibitor (BT#9) effects on prostate cancer and examined the molecular mechanism of BT#9. A cell viability assay ... ...

Abstract	The purpose of our study was to evaluate Magmas as a potential target in prostate cancer. In addition, we evaluated our synthetic Magmas inhibitor (BT#9) effects on prostate cancer and examined the molecular mechanism of BT#9. A cell viability assay showed that treatment with BT#9 caused a significant decrease in the viability of DU145 and PC3 prostate cancer cells with little effect on the viability of WPMY-1 normal prostate cells. Western blot proved that BT#9 downregulated the Magmas protein and caspase-3 activation. Flow cytometry studies demonstrated increased apoptosis and disturbed mitochondrial membrane potential. However, the main mode of cell death was caspase-independent necrosis, which was correlated with the accumulation of mitochondrial and intra-cellular Reactive Oxygen Species (ROS). Taken together, our data suggest Magmas is a potential molecular target for the treatment of prostate cancer and that Magmas inhibition results in ROS-dependent and caspase-independent necrotic cell death.
Language	English
Publishing date	2022-05-31
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2527080-1
ISSN	2072-6694
ISSN	2072-6694
DOI	10.3390/cancers14112732
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Article: Synthesis of a boron-containing amidoxime reagent and its application to synthesize functionalized oxadiazole and quinazolinone derivatives.

Das, Bhaskar C / Nandwana, Nitesh K / Ojha, Devi P / Das, Sasmita / Evans, Todd

Tetrahedron letters

2022 Volume 92

Abstract	Herein, we report the design, synthesis and application of a borylated amidoxime reagent for the direct synthesis of functionalized oxadiazole and quinazolinone derivatives. This reagent exhibits broad synthetic utility to obtain a variety of biologically relevant drug-like molecules. It can be easily prepared at large scale from relatively inexpensive reagents, and can undergo facile transformations to obtain target compounds. The developed amidoxime reagent was synthesized from 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile and hydroxyl amine hydrochloride using
Language	English
Publishing date	2022-01-25
Publishing country	England
Document type	Journal Article
ZDB-ID	204287-3
ISSN	1873-3581 ; 0040-4039
ISSN (online)	1873-3581
ISSN	0040-4039
DOI	10.1016/j.tetlet.2022.153657
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Zs.A 2837: Show issues

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Jg. 1995 - 2021: Lesesall (2.OG)
ab Jg. 2022: Lesesaal (EG)

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Article: Effects of retinoic acid receptor α modulators on developmental ethanol-induced neurodegeneration and neuroinflammation.

Saito, Mariko / Subbanna, Shivakumar / Zhang, Xiuli / Canals-Baker, Stefanie / Smiley, John F / Wilson, Donald A / Das, Bhaskar C

Frontiers in neuroscience

2023 Volume 17, Page(s) 1170259

Abstract: Ethanol exposure in neonatal mice induces acute neurodegeneration followed by long-lasting glial activation and GABAergic cell deficits along with behavioral abnormalities, providing a third trimester model of fetal alcohol spectrum disorders (FASD). ... ...

Abstract	Ethanol exposure in neonatal mice induces acute neurodegeneration followed by long-lasting glial activation and GABAergic cell deficits along with behavioral abnormalities, providing a third trimester model of fetal alcohol spectrum disorders (FASD). Retinoic acid (RA), the active form of vitamin A, regulates transcription of RA-responsive genes and plays essential roles in the development of embryos and their CNS. Ethanol has been shown to disturb RA metabolism and signaling in the developing brain, which may be a cause of ethanol toxicity leading to FASD. Using an agonist and an antagonist specific to RA receptor α (RARα), we studied how RA/RARα signaling affects acute and long-lasting neurodegeneration and activation of phagocytic cells and astrocytes caused by ethanol administered to neonatal mice. We found that an RARα antagonist (BT382) administered 30 min before ethanol injection into postnatal day 7 (P7) mice partially blocked acute neurodegeneration as well as elevation of CD68-positive phagocytic cells in the same brain area. While an RARα agonist (BT75) did not affect acute neurodegeneration, BT75 given either before or after ethanol administration ameliorated long-lasting astrocyte activation and GABAergic cell deficits in certain brain regions. Our studies using Nkx2.1-Cre;Ai9 mice, in which major GABAergic neurons and their progenitors in the cortex and the hippocampus are labeled with constitutively expressed tdTomato fluorescent protein, indicate that the long-lasting GABAergic cell deficits are mainly caused by P7 ethanol-induced initial neurodegeneration. However, the partial reduction of prolonged GABAergic cell deficits and glial activation by post-ethanol BT75 treatment suggests that, in addition to the initial cell death, there may be delayed cell death or disturbed development of GABAergic cells, which is partially rescued by BT75. Since RARα agonists including BT75 have been shown to exert anti-inflammatory effects, BT75 may rescue GABAergic cell deficits by reducing glial activation/neuroinflammation.
Language	English
Publishing date	2023-05-02
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2411902-7
ISSN	1662-453X ; 1662-4548
ISSN (online)	1662-453X
ISSN	1662-4548
DOI	10.3389/fnins.2023.1170259
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Article ; Online: Anti-inflammatory Action of BT75, a Novel RARα Agonist, in Cultured Microglia and in an Experimental Mouse Model of Alzheimer's Disease.

Zhang, Xiuli / Subbanna, Shivakumar / Williams, Colin R O / Canals-Baker, Stefanie / Smiley, John F / Wilson, Donald A / Das, Bhaskar C / Saito, Mariko

Neurochemical research

2023 Volume 48, Issue 6, Page(s) 1958–1970

Abstract: BT75, a boron-containing retinoid, is a novel retinoic acid receptor (RAR)α agonist synthesized by our group. Previous studies indicated that activation of retinoic acid (RA) signaling may attenuate progression of Alzheimer's disease (AD). Presently, we ... ...

Abstract	BT75, a boron-containing retinoid, is a novel retinoic acid receptor (RAR)α agonist synthesized by our group. Previous studies indicated that activation of retinoic acid (RA) signaling may attenuate progression of Alzheimer's disease (AD). Presently, we aimed to examine the anti-inflammatory effect of BT75 and explore the possible mechanism using cultured cells and an AD mouse model. Pretreatment with BT75 (1-25 µM) suppressed the release of nitric oxide (NO) and IL-1β in the culture medium of mouse microglial SIM-A9 cells activated by LPS. BMS195614, an RARα antagonist, partially blocked the inhibition of NO production by BT75. Moreover, BT75 attenuated phospho-Akt and phospho-NF-κB p65 expression augmented by LPS. In addition, BT75 elevated arginase 1, IL-10, and CD206, and inhibited inducible nitric oxide synthase (iNOS) and IL-6 formation in LPS-treated SIM-A9 cells, suggesting the promotion of M1-M2 microglial phenotypic polarization. C57BL/6 mice were injected intracerebroventricularly (icv) with streptozotocin (STZ) (3 mg/kg) to provide an AD-like mouse model. BT75 (5 mg/kg) or the vehicle was intraperitoneally (ip) injected to icv-STZ mice once a day for 3 weeks. Immunohistochemical analyses indicated that GFAP-positive cells and rod or amoeboid-like Iba1-positive cells, which increased in the hippocampal fimbria of icv-STZ mice, were reduced by BT75 treatment. Western blot results showed that BT75 decreased levels of neuronal nitric oxide synthase (nNOS), GFAP, and phosphorylated Tau, and increased levels of synaptophysin in the hippocampus of icv-STZ mice. BT75 may attenuate neuroinflammation by affecting the Akt/NF-κB pathway and microglial M1-M2 polarization in LPS-stimulated SIM-A9 cells. BT75 also reduced AD-like pathology including glial activation in the icv-STZ mice. Thus, BT75 may be a promising anti-inflammatory and neuroprotective agent worthy of further AD studies.
MeSH term(s)	Mice ; Animals ; Microglia/metabolism ; NF-kappa B/metabolism ; Alzheimer Disease/chemically induced ; Alzheimer Disease/drug therapy ; Alzheimer Disease/metabolism ; Lipopolysaccharides/toxicity ; Proto-Oncogene Proteins c-akt/metabolism ; Mice, Inbred C57BL ; Anti-Inflammatory Agents/pharmacology ; Anti-Inflammatory Agents/therapeutic use
Chemical Substances	NF-kappa B ; Lipopolysaccharides ; Proto-Oncogene Proteins c-akt (EC 2.7.11.1) ; Anti-Inflammatory Agents
Language	English
Publishing date	2023-02-13
Publishing country	United States
Document type	Journal Article
ZDB-ID	199335-5
ISSN	1573-6903 ; 0364-3190
ISSN (online)	1573-6903
ISSN	0364-3190
DOI	10.1007/s11064-023-03888-x
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