Pharmaceutical Sciences and Natural Products - Research Publications

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1-Acetyl-3, 5?diaryl-4, 5?dihydro (1H) pyrazoles: Exhibiting Anticancer Activity through Intracellular ROS Scavenging and the Mitochondria-Dependent Death Pathway
(Wiley, 2014) Alex, JM; Singh, S; Kumar, Raj
A series of 17 analogs of 1?acetyl?4,5?dihydro(1H)pyrazoles (JP?1 to JP?17) bearing two aromatic rings at positions 3 and 5, either of which ought to be heterocyclic, were synthesized and evaluated for their anti?proliferative potential against breast cancer (MCF?7 and T?47D) and lung cancer (H?460 and A?549) cell lines for the first time.JP-1–7, -10, -11, -14, and ?15 were observed to exhibit significant anti?proliferative activity against MCF?7 cells. Some notions about structure - activity relationships are reported. The investigated compounds were found to lower the intracellular reactive oxygen species in the H2DCFDA assay and also caused mitochondria?dependent cell death in the MCF?7 cell line, indicating a plausible mechanism of their anticancer effect.
1-Acetyl-3,5-diaryl-4,5-dihydro(1H)pyrazoles: Exhibiting anticancer activity through intracellular ROS scavenging and the mitochondria-dependent death pathway
(Wiley-VCH Verlag, 2014) Alex, Jimi M.; Singh, Sandeep; Kumar, Raj
A series of 17 analogs of 1-acetyl-4,5-dihydro(1H)pyrazoles (JP-1 to JP-17) bearing two aromatic rings at positions 3 and 5, either of which ought to be heterocyclic, were synthesized and evaluated for their anti-proliferative potential against breast cancer (MCF-7 and T-47D) and lung cancer (H-460 and A-549) cell lines for the first time. JP-1-7, -10, -11, -14, and -15 were observed to exhibit significant anti-proliferative activity against MCF-7 cells. Some notions about structure-activity relationships are reported. The investigated compounds were found to lower the intracellular reactive oxygen species in the H2DCFDA assay and also caused mitochondria-dependent cell death in the MCF-7 cell line, indicating a plausible mechanism of their anticancer effect. Analogs of 1-acetyl-4,5-dihydro(1H)pyrazoles (JP-1-17) were synthesized and evaluated for their anti-proliferative activity in four cancer cell lines and for their intracellular ROS scavenging properties. An attempt was made to determine the mitochondrial membrane potential of MCF-7 cells treated with JP-1 and -14, aiming to elucidate the mechanism by which proliferation was curbed. ? 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
2-(2-Arylphenyl) benzoxazole As a Novel Anti-Inflammatory Scaffold: Synthesis and Biological Evaluation
(ACS publications, 2014) Seth, Kapileswar; Garg, Sanjeev K.; Kumar, Raj; Purohit, Priyank; Meena, Vachan S.; Goyal, Rohit; Banerjee, Uttam C.; Chakraborti, Asit K.
The 2-(2-arylphenyl)benzoxazole moiety has been found to be a new and selective ligand for the enzyme cyclooxygenase-2 (COX-2). The 2-(2-arylphenyl)benzoxazoles 3a−m have been synthesized by Suzuki reaction of 2-(2-bromophenyl)benzoxazole. Further synthetic manipulation of 3f and 3i led to 3o and 3n, respectively. The compounds 3g, 3n, and 3o selectively inhibited COX-2 with selectivity index of 3n much better than that of the COX-2 selective NSAID celecoxib. The in vivo anti-inflammatory potency of 3g and 3n is comparable to that of celecoxib and the nonselective NSAID diclofenac at two different doses, and 3o showed better potency compared to these clinically used NSAIDs.
4,5-Dihydro-1H-pyrazole: An indispensable scaffold
(Informa Healthcare, 2014) Alex, Jimi Marin; Kumar, Raj
Pyrazoles, categorized as nitrogen-containing heterocycles, are well known for their interminable participation in the field of perpetual research and development of therapeutical active agents. As a consequence pyrazoles became an inevitable core of numerous drugs having diverse activities. The broad spectrum of activities portrayed by the pyrazoles instigated the researchers to modify the pyrazole ring as 4,5-dihydro-1H-pyrazoles commonly known as 2-pyrazolines. The present review is a concerted effort to retrace compounds covered from 2009-till date which owe diverse biological activities to the 2-pyrazoline scaffold and also condenses the retro-synthetic approaches employed for their synthesis. This endeavor culminated in revelation that inhibitory potential varied when the substituents in particular N-substituents of 2-pyrazolines were altered. ? 2014 Informa UK Ltd.
4,6-Diphenylpyrimidine Derivatives as Dual Inhibitors of Monoamine Oxidase and Acetylcholinesterase for the Treatment of Alzheimer's Disease
(American Chemical Society, 2019) Kumar, B; Dwivedi, A.R; Sarkar, B; Gupta, S.K; Krishnamurthy, S; Mantha, Anil K; Parkash, Jyoti; Kumar, Vinod
Alzheimer's disease (AD) is a neurodegenerative disorder with multifactorial pathogenesis. Monoamine oxidase (MAO) and acetylcholinesterase enzymes (AChE) are potential targets for the treatment of AD. A total of 15 new propargyl containing 4,6-diphenylpyrimidine derivatives were synthesized and screened for the MAO and AChE inhibition activities along with ROS production inhibition and metal-chelation potential. All the synthesized compounds were found to be selective and potent inhibitors of MAO-A and AChE enzymes at nanomolar concentrations. VB1 was found to be the most potent MAO-A and BuChE inhibitor with IC 50 values of 18.34 ± 0.38 nM and 0.666 ± 0.03 μM, respectively. It also showed potent AChE inhibition with an IC 50 value of 30.46 ± 0.23 nM. Compound VB8 was found to be the most potent AChE inhibitor with an IC 50 value of 9.54 ± 0.07 nM and displayed an IC 50 value of 1010 ± 70.42 nM against the MAO-A isoform. In the cytotoxic studies, these compounds were found to be nontoxic to the human neuroblastoma SH-SY5Y cells even at 25 μM concentration. All the compounds were found to be reversible inhibitors of MAO-A and AChE enzymes. In addition, these compounds also showed good neuroprotective properties against 6-OHDA- and H 2 O 2 -induced neurotoxicity in SH-SY5Y cells. All the compounds accommodate nicely to the hydrophobic cavity of MAO-A and AChE enzymes. In the molecular dynamics simulation studies, both VB1 and VB8 were found to be stable in the respective cavities for 30 ns. Thus, 4,6-diphenylpyrimidine derivatives can act as promising leads in the development of dual-acting inhibitors targeting MAO-A and AChE enzymes for the treatment of Alzheimer's disease. © 2018 American Chemical Society.
Accumulated polymer degradation products as effector molecules in cytotoxicity of polymeric nanoparticles
(2013) Singh, R.P.; Ramarao, P.
Polymeric nanoparticles (PNPs) are a promising platform for drug, gene, and vaccine delivery. Although generally regarded as safe, the toxicity of PNPs is not well documented. The present study investigated in vitro toxicity of poly-?-caprolactone, poly(DL-lactic acid), poly(lactide-cocaprolactone), and poly(lactide-co-glycide) NPs and possible mechanism of toxicity. The concentration-dependent effect of PNPs on cell viability was determined in a macrophage (RAW 264.7), hepatocyte (Hep G2), lung epithelial (A549), kidney epithelial (A498), and neuronal (Neuro 2A) cell lines. PNPs show toxicity at high concentrations in all cell lines. PNPs were efficiently internalized by RAW 264.7 cells and stimulated reactive oxygen species and tumor necrosis factor-alpha production. However, reactive nitrogen species and interleukin-6 production as well as lysosomal and mitochondrial stability remained unaffected. The intracellular degradation of PNPs was determined by monitoring changes in osmolality of culture medium and a novel fluorescence recovery after quenching assay. Cell death showed a good correlation with osmolality of culture medium suggesting the role of increased osmolality in cell death. ? The Author 2013. Published by Oxford University Press on behalf of the Society of Toxicology. All rights reserved.
Alzheimer's disease: Molecular aspects and treatment opportunities using herbal drugs
(Elsevier Ireland Ltd, 2023-05-22T00:00:00) Thakral, Samridhi; Yadav, Alka; Singh, Vikramjeet; Kumar, Manoj; Kumar, Pradeep; Narang, Rakesh; Sudhakar, Kalvatala; Verma, Amita; Khalilullah, Habibullah; Jaremko, Mariusz; Emwas, Abdul-Hamid
Alzheimer's disease (AD), also called senile dementia, is the most common neurological disorder. Around 50 million people, mostly of advanced age, are suffering from dementia worldwide and this is expected to reach 100�130 million between 2040 and 2050. AD is characterized by impaired glutamatergic and cholinergic neurotransmission, which is associated with clinical and pathological symptoms. AD is characterized clinically by loss of cognition and memory impairment and pathologically by senile plaques formed by Amyloid ? deposits or neurofibrillary tangles (NFT) consisting of aggregated tau proteins. Amyloid ? deposits are responsible for glutamatergic dysfunction that develops NMDA dependent Ca2+ influx into postsynaptic neurons generating slow excitotoxicity process leading to oxidative stress and finally impaired cognition and neuronal loss. Amyloid decreases acetylcholine release, synthesis and neuronal transport. The decreased levels of neurotransmitter acetylcholine, neuronal loss, tau aggregation, amyloid ? plaques, increased oxidative stress, neuroinflammation, bio-metal dyshomeostasis, autophagy, cell cycle dysregulation, mitochondrial dysfunction, and endoplasmic reticulum dysfunction are the factors responsible for the pathogenesis of AD. Acetylcholinesterase, NMDA, Glutamate, BACE1, 5HT6, and RAGE (Receptors for Advanced Glycation End products) are receptors targeted in treatment of AD. The FDA approved acetylcholinesterase inhibitors Donepezil, Galantamine and Rivastigmine and N-methyl-D-aspartate antagonist Memantine provide symptomatic relief. Different therapies such as amyloid ? therapies, tau-based therapies, neurotransmitter-based therapies, autophagy-based therapies, multi-target therapeutic strategies, and gene therapy modify the natural course of the disease. Herbal and food intake is also important as preventive strategy and recently focus has also been placed on herbal drugs for treatment. This review focuses on the molecular aspects, pathogenesis and recent studies that signifies the potential of medicinal plants and their extracts or chemical constituents for the treatment of degenerative symptoms related to AD. � 2023 Elsevier B.V.
Amino Acid Derived Prodrugs: An Approach to Improve the Bioavailability of Clinically Approved Drugs
(Bentham Science Publishers, 2021-06-04T00:00:00) Singh, Yogesh; Saklani, Samriti; Tantra, Tanmoy; Thareja, Suresh
Amino acids derived prodrugs emerged as an attractive approach to improve oral delivery of drugs with low solubility and permeability. Conjugation of amino acids with parent drug molecules resulted in several-fold increases in water solubility. Acceptability of the amino acids derived prodrug approach increases day by day to fulfill the different characteristics needed to get the desired pharmacological or therapeutic activity. Due to the significant structural diversity of amino acids, various amino acids can be employed as a carrier to provide desirable Pharmacokinetic-Phar-macodynamic (PK-PD) characteristics. The present review focused on using amino acids as a carrier moiety to improve approved drugs' bioavailability. Attempts have been made to cover amino acid conjugated clinically available drugs. � 2021 Bentham Science Publishers.
Anticancer activity of dihydropyrazolo [1, 5‐c] quinazolines against rat C6 glioma cells via inhibition of topoisomerase II
(wiley, 2018) Kaur, G; Cholia, Raman Preet; Joshi, G; Amrutkar, S.M; Kalra, S; Mantha, Anil K.; Banerjee, U.C; Kumar, R.
The design and synthesis of dihydropyrazolo[1,5‐c]quinazolines (1a–h) as human topoisomerase II (TopoII) catalytic inhibitors are reported. The compounds were investigated for their antiproliferative activity against the C6 rat glial cell line. Two compounds, 1b and 1h, were found to be potent cytotoxic agents against glioma cells and exerted selective TopoII inhibitory activity. Furthermore, the compounds induced alterations in reactive oxygen species levels as measured by DCFDA assay and were found to induce cell cycle arrest at the G1 phase at lower concentrations and profound apoptosis at higher concentrations. The interaction of selected investigational molecules with TopoII was further corroborated by molecular modeling
Anticancer activity of dihydropyrazolo[1,5-c]quinazolines against rat C6 glioma cells via inhibition of topoisomerase II
(Wiley-VCH Verlag, 2018) Kaur, G.; Cholia, R.P.; Joshi, G.; Amrutkar, S.M.; Kalra, S.; Mantha, Anil K.; Banerjee, U.C.; Kumar, Raj
The design and synthesis of dihydropyrazolo[1,5-c]quinazolines (1a?h) as human topoisomerase II (TopoII) catalytic inhibitors are reported. The compounds were investigated for their antiproliferative activity against the C6 rat glial cell line. Two compounds, 1b and 1h, were found to be potent cytotoxic agents against glioma cells and exerted selective TopoII inhibitory activity. Furthermore, the compounds induced alterations in reactive oxygen species levels as measured by DCFDA assay and were found to induce cell cycle arrest at the G1 phase at lower concentrations and profound apoptosis at higher concentrations. The interaction of selected investigational molecules with TopoII was further corroborated by molecular modeling. ? 2018 Deutsche Pharmazeutische Gesellschaft
Anticancer activity of essential oils: A review
(2013) Bhalla, Yashika; Gupta, Vinay Kumar; Jaitak, Vikas
Natural essential oil constituents play an important role in cancer prevention and treatment. Essential oil constituents from aromatic herbs and dietary plants include monoterpenes, sesquiterpenes, oxygenated monoterpenes, oxygenated sesquiterpenes and phenolics among others. Various mechanisms such antioxidant, antimutagenic and antiproliferative, enhancement of immune function and surveillance, enzyme induction and enhancing detoxification, modulation of multidrug resistance and synergistic mechanism of volatile constituents are responsible for their chemopreventive properties. This review covers the most recent literature to summarize structural categories and molecular anticancer mechanisms of constituents from aromatic herbs and dietary plants. ? 2013 Society of Chemical Industry.
Antimicrobial and repellent activity of the essential oils of two lamiaceae cultivated in Western Himalaya
(Bentham Science Publishers B.V., 2015) Stappen, Iris; Ali, Abbas; Tabanca, Nurhayat; Khan,Ikhlas A.; Wanner, J�rgen; Gochev, Velizar K.; Singh, Virendra; Lal, Brij; Jaitak, Vikas; Kaul, Vijay K.; Schmidt, Erich; Jirovetz, Leopold; Stappen, I.; Ali, A.; Tabanca, N.; Khan, I.A.; Wanner, J.; Gochev, V.K.; Singh, V.; Lal, B.; Jaitak, V.; Kaulh, V.K.; Schmidt, E.; Jirovetz, L.
The essential oils of two Lamiaceae cultivated in Western Himalaya were examined on their antimicrobial, biting deterrent as well as larvicidal activity. Additionally their odors are described and their chemical compositions analyzed by GC-MS are given. The main component of Nepeta cataria oil was 4a?,7?,7a?-nepetalactone (85%), whereas camphor (27%) and 1,8-cineol (27%) were dominant in the oil of Rosmarinus officinalis. The studied essential oils demonstrated high to moderately antimicrobial activity against reference strains, clinical and food spoilage isolates of Bacillus cereus, Staphylococcus aureus, Escherichia coli, Salmonella abony and Candida albicans (MIC 160-640 ?g/ml) and indicated low activity against Pseudomonas aeruginosa and P. fluorescens. Both oils showed biting deterrent activity above solvent control but lower than DEET. Nepeta catarica essential oil exhibited high toxicity with LD50 value of 20.2 whereas R. officinalis oil showed only 50% mortality at the highest tested dose of 125 ppm against 1-day old Aedes aegypti larvae at 24-hour post treatment. ? 2015 Bentham Science Publishers.
Applications of dihydropyrimidinone derivatives on blood cancer and colon cancer
(Elsevier, 2023-08-25T00:00:00) Singh, Ankit Kumar; Singh, Harshwardhan; Sonawane, Pankaj; Kumar, Adarsh; Verma, Amita; Kumar, Pradeep
Dihydropyrimidinones (DHPMs) are characterized by their multifunctionalized scaffold with a pyrimidine moiety that exhibits diverse biological activities, especially anticancer activity. Malignant clonal expansion of blood-forming cells is referred to as blood cancer. Colorectal cancer (CRC) appears within the colon or another bodily area. There were 9,958,133 fatalities and 19,292,789 new cases of 36 cancers globally in 2020. In this, 1,148,515 cases and 576,858 deaths belong to colon cancer, whereas 474,519 cases and 311,594 deaths belong to leukemia. Different blood cancer cell lines, such as MOLT-4, HL-60, CCRF-CEMT, K-562, U937, MOLT-4, RPMI-8226, THP-1, and SR, as well as colon cancer/CRC cell lines, HCT-116, HCT-15, Colo205, HCC-2998, HCT-116, HT-29, KM-12, and SW-620, have been used to evaluate in vitro anticancer activity of DHPM derivatives. DHPM derivatives demonstrated notable effectiveness against blood and colon/colorectal cancers and may prove important building blocks in the development of novel anticancer agents. � 2023 Elsevier Inc. All rights reserved.
Asparagus racemosus (Shatavari) targeting estrogen receptor a: - An in-vitro and in-silico mechanistic study
(Taylor and Francis Ltd., 2018) Sharma R.; Jaitak V.
Breast cancer is a disease where cells in the tissue of the breast, grow and divide without normal control. Breast cancer is second major cause for death in world wide. Importance of natural product increase due to adverse effect of existing synthetic drugs. Asparagus racemosus comprises phytoestrogens which can be used for the treatment of breast cancer. In the current study, In vitro antiproliferative activity of the extracts of A. racemosus is performed in T47D cancer cell lines. Outcomes of the result indicated that aqueous methanol and methanol extract showed excellent antiproliferative activity as compared to bazedoxifene (standard), ethyl acetate and petroleum ether extract. In silico study of reported phytochemical constituents of A. racemosus was performed for understand the molecular mechanism and prospect pharmacophore development. Furthermore, compound 26 (rutin) which has been earlier reported and isolated from alcoholic extract exhibited the remarkable binding profile with estrogen receptor ?. For that reason, our study proposed that A. racemosus could be used as a new source for the treatment of breast cancer.
Association of CYP2C19*2 and ALDH1A1*1/*2 variants with disease outcome in breast cancer patients: results of a global screening array.
(Springer, 2018) Kalra, Sourav; Ludhiadch Abhilash; Shafi, Gowhar; Vashista, Rajesh; Kumar, Raj; Munshi, Anjana
Cyclophosphamide and doxorubicin (adjuvant chemotherapy) are commonly used to treat breast cancer patients. Variation in the genes involved in pharmacodynamics and pharmacokinetics of these drugs plays an important role in prediction of drug response and survival. The present study was carried out with an aim to evaluate the variation in all the genes involved in pharmacokinetic and pharmacodynamics pathways of cyclophosphamide and doxorubicin, and correlate specific variants with disease outcome in breast cancer patients from the Malwa region of Punjab.
Augmented anticancer efficacy of doxorubicin-loaded polymeric nanoparticles after oral administration in a breast cancer induced animal model
(2011) Jain, A.K.; Swarnakar, N.K.; Das, M.; Godugu, C.; Singh, R.P.; Rao, P.R.; Jain, S.
The present investigation reports an extensive evaluation of in vitro and in vivo anticancer efficacy of orally administered doxorubicin-loaded poly(lactic-co-glycolic acid) (PLGA) nanoparticles (Dox-NPs) in a breast cancer induced animal model. Spherically shaped Dox-NPs were prepared with an entrapment efficiency and particle size of 55.40 ? 2.30% and 160.20 ? 0.99 nm, respectively, and freeze-dried with 5% trehalose using stepwise freeze-drying. Cytotoxicity, as investigated on C127I cell line, revealed insignificant differences between the IC 50 of free Dox and Dox-NPs treated cells in the first 24 h, while higher cytotoxicity was demonstrated by Dox-NPs, following 72 h of incubation. Confocal laser scanning microscopy (CLSM) imaging corroborated that nanoparticles were efficiently localized into the nuclear region of C127I cells. The cellular uptake profile of Dox-NPs revealed both time and concentration dependent increases in the Caco-2 cell uptake as compared to the free Dox solution. Further, Dox-NPs significantly suppressed the growth of breast tumor in female Sprague-Dawley (SD) rats upon oral administration. Finally, orally administered Dox-NPs showed a marked reduction in cardiotoxicity when compared with intravenously injected free Dox as also evident by the increased level of malondialdehyde (MDA), lactate dehydrogenase (LDH), and creatine phosphokinase (CK-MB) and reduced levels of glutathione (GSH) and superoxide dismutase (SOD). The reduced cardiotoxicity of orally administered Dox-NPs was also confirmed by the major histopathological changes in the heart tissue after the treatments of intravenously injected free Dox and orally delivered Dox-NPs. ? 2011 American Chemical Society.
Bacteriophages Concept and Applications: A Review on Phage Therapy
(Bentham Science Publishers, 2022-11-07T00:00:00) Sahu, Rasti; Singh, Ankit Kumar; Kumar, Adarsh; Singh, Kuldeep; Kumar, Pradeep
The nature of phages was a matter of dispute, which was resolved in 1940, and it was continued to develop their activity and application in the Soviet Union and Eastern Europe. Bacterio-phages were first employed in 1919 to treat bacterial illnesses caused by Citrobacter, Enterobacter, and Pseudomonas. Bacteriophages range in complexity from simple spherical viruses with genome sizes of less than 5 kbp to complicated viruses with genome sizes surpassing 280 kbp. They have two significant parts, head and tail, and are made up of numerous copies of more than 40 distinct proteins. Bacteriophages have been demonstrated to bind with receptors in the walls of both gram-positive and gram-negative bacteria, ranging from peptide sequences to polysaccharide moieties. Depending on the type of phage and the physiological state of the bacterium, the life cycle may diverge into the lytic cycle or lysogenic cycle. Lytic-lysogenic switch depends on a variety of inducing factors. Bacteriophage therapy can be administered via several routes, but parenteral routes are the most effec-tive. Auto-dosing, single-dose potential, lack of cross-resistance with antibiotics, etc., are several advantages of phage therapy over antibiotic treatment. Bacteriophages are attracting much attention because of their potential advantages and wide applications as antibacterial agents, diagnostic technolo-gies, phage-based products, and biocontrol agents. They also have several applications in the food industry, agriculture/crop, farm animal and bee protection, environmental, and biosensor development. � 2023 Bentham Science Publishers.
Bioanalytical Applications of Graphene Quantum Dots for Circulating Cell-Free Nucleic Acids: A Review
(American Chemical Society, 2022-10-26T00:00:00) Ratre, Pooja; Jain, Bulbul; Kumari, Roshani; Thareja, Suresh; Tiwari, Rajnarayan; Srivastava, Rupesh Kumar; Goryacheva, Irina Yu; Mishra, Pradyumna Kumar
Graphene quantum dots (GQDs) are carbonaceous nanodots that are natural crystalline semiconductors and range from 1 to 20 nm. The broad range of applications for GQDs is based on their unique physical and chemical properties. Compared to inorganic quantum dots, GQDs possess numerous advantages, including formidable biocompatibility, low intrinsic toxicity, excellent dispensability, hydrophilicity, and surface grating, thus making them promising materials for nanophotonic applications. Owing to their unique photonic compliant properties, such as superb solubility, robust chemical inertness, large specific surface area, superabundant surface conjugation sites, superior photostability, resistance to photobleaching, and nonblinking, GQDs have emerged as a novel class of probes for the detection of biomolecules and study of their molecular interactions. Here, we present a brief overview of GQDs, their advantages over quantum dots (QDs), various synthesis procedures, and different surface conjugation chemistries for detecting cell-free circulating nucleic acids (CNAs). With the prominent rise of liquid biopsy-based approaches for real-time detection of CNAs, GQDs-based strategies might be a step toward early diagnosis, prognosis, treatment monitoring, and outcome prediction of various non-communicable diseases, including cancers. � 2022 American Chemical Society. All rights reserved.
Boron in cancer therapeutics: An overview
(Elsevier Inc., 2023-10-17T00:00:00) Kulkarni, Swanand; Bhandary, Dyuti; Singh, Yogesh; Monga, Vikramdeep; Thareja, Suresh
Boron has become a crucial weapon in anticancer research due to its significant intervention in cell proliferation. Being an excellent bio-isosteric replacement of carbon, it has modulated the anticancer efficacy of various molecules in the development pipeline. It has elicited promising results through interactions with various therapeutic targets such as HIF-1?, steroid sulfatase, arginase, proteasome, etc. Since boron liberates alpha particles, it has a wide-scale application in Boron Neutron Capture therapy (BNCT), a radiotherapy that demonstrates selectivity towards cancer cells due to high boron uptake capacity. Significant advances in the medicinal chemistry of boronated compounds, such as boronated sugars, natural/unnatural amino acids, boronated DNA binders, etc., have been reported over the past few years as BNCT agents. In addition, boronated nanoparticles have assisted the field of bio-nano medicines by their usage in radiotherapy. This review exclusively focuses on the medicinal chemistry aspects, radiotherapeutic, and chemotherapeutic aspects of boron in cancer therapeutics. Emphasis is also given on the mechanism of action along with advantages over conventional therapies. � 2023 Elsevier Inc.
C‐N and N‐N bond formation via Reductive Cyclization: Progress in Cadogan /Cadogan‐Sundberg Reaction.
(wiley, 2018) Kaur, Manpreet; Kumar, Raj Kumar
Cadogan/Cadogan‐Sundberg cyclization reaction has been reported as one of the most efficient routes for the synthesis of a wide variety of N‐heterocycles from the easily accessible starting materials such as o‐nitrobiaryls or o‐nitroarenes, o‐nitrostyrenes by treating with tetravalent phosphorus compounds (trialkyl or triaryl phosphines or trialkyl phosphites). The reaction has been successfully employed in Carbon‐Carbon as well as Carbon‐Nitrogen bond formation for the scaffolds like carbazole, indoles, coumarins, and indazoles. To the best of authors’ knowledge, the present review is the first compilation of the literature from almost two decades (2000 to present) on Cadogan/Cadogan‐Sundberg cyclization reaction, its scope, mechanistic aspects, and limitations.