School Of Basic And Applied Sciences

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Author: search.filters.author.Kumar, RajSubject: search.filters.subject.Synthesis

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Now showing 1 - 9 of 9
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    FDA approved five-membered ring fused pyrimidine-based derivatives and their biological properties
    (Elsevier, 2022-10-14T00:00:00) Kumar, Manvendra; Chatterjee, Joydeep; Rani, Dimpy; Kumar, Raj
    Pyrimidines-based drugs are one of the most important drugs for novel and recurring viruses, including the coronavirus. This chapter deals with 41 FDA-approved five-membered ring fused pyrimidine-based drugs, their synthetic strategies, and pharmacological activities. � 2023 Elsevier Ltd. All rights reserved.
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    FDA approved six-membered ring fused pyrimidine-based derivatives
    (Elsevier, 2022-10-14T00:00:00) Arora, Sahil; Kumar, Raj
    Pyrimidine-based derivatives play a vital role in the development of drugs due to their indispensable role in various biological processes. To date, ring fused pyrimidine-based derivatives have been reported to exhibit numerous biological activities including anticancer, antiviral, antianginal, anti-HIV, antifungal, antibacterial, anti-inflammatory, antitubercular and many others. There are numerous synthetic approaches available for the synthesis of fused pyrimidine-based derivatives which provides ample scope in the development of new drugs. Considering these medicinal attributes of fused pyrimidine-based derivatives, we have put forth this book chapter mainly focusing on the FDA approved six-membered ring fused pyrimidine-based derivatives. The present chapter deals with improved synthetic schemes, their biological importance and the adverse effects of FDA approved six-membered ring fused pyrimidine-based drugs. Covering all these aspects may lighten the researchers with the updated literature exploring the best synthetic routes and can think of alternative synthetic routes with less time consuming and non-toxic solvents. � 2023 Elsevier Ltd. All rights reserved.
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    Melphalan: Recent insights on synthetic, analytical and medicinal aspects
    (Elsevier Masson s.r.l., 2022-05-27T00:00:00) Pahwa, Rakesh; Chhabra, Jatin; Kumar, Raj; Narang, Rakesh
    Cancer is an uncontrolled expansion of atypical cells in the body. These unusual cells are labelled as cancerous or malignant cells. Melphalan, an anticancer drug which is imperatively recognized under the class of alkylating agents. It exhibits broad spectrum antitumor activity, as observed in ovarian cancer, breast cancer, etc. However, it is mainly utilized in the management of multiple myeloma. Several studies across the globe suggest that resistance to melphalan is the major concern that leads to relapsed myeloma. In the present paper, several pivotal approaches to compensate resistance associated with melphalan have been discussed. Numerous chemical and formulation developments concerning melphalan to enhance its salient characteristics and targeted profile have also been portrayed. The rationale of the current article also summarizes the recent analytical methods, structure-activity relationship, pharmacokinetics, interactions, potential adverse effects along with medicinal updates of melphalan. Special attention is also laid on their synthetic developments viz. melphalan derivatives, conjugates and prodrugs along with encouraging insights and research findings. � 2022 Elsevier Masson SAS
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    Synthetic strategies and pharmacological activities of chromene and its derivatives: An overview
    (Elsevier B.V., 2022-04-07T00:00:00) Katiyar, Madhurendra K.; Dhakad, Govind Kumar; Shivani; Arora, Sahil; Bhagat, Srikant; Arora, Taruna; Kumar, Raj
    Chromene is commonly found in nature and is considered one of the most frequently used scaffolds in heterocyclic chemistry for the designing of chemical probes for therapeutic and diagnostic purposes. The chromene nucleus comprises an oxine ring fused with a phenyl ring. Owing to existing several useful biological applications of chromenes have generated wide interest among chemists to synthesize its derivatives frequently. Here, in this review, we have compiled and analysed various recently reported synthetic strategies of chromene and its derivatives through numerous approaches such as microwave-assisted, catalyst based, green solvents, solvent-free conditions, etc. along with their biological applications such as anticancer, antimicrobial, anti-inflammatory, AChE inhibition, antiviral, and antioxidant activities. � 2022 Elsevier B.V.
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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.
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    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.
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    Pyrazoloquinazolines: Synthetic strategies and bioactivities
    (2015) Garg, Mansi; Chauhan, Monika; Singh, Pankaj Kumar; Singh, Pankaj Kumar; Alex, Jimi Marin; Kumar, Raj
    Numerous N-heterocycles are indisputably evidenced to exhibit myriad biological activities. In the recent past, attempts made to condense the various heterocycles have resulted in derivatives possessing better bioactivities. Among many such condensed heterocycles, pyrazoloquinazolines have managed to hold the attention of many researchers, owing to the broad spectrum of activities they portray. This review is the first of its kind to congregate the various pyrazoloquinazolines reported until now and categorizes these structurally isomeric classes into eleven different groups based on the fusion pattern of the ring such as [1,5-c], [5,1-b], [4,3-h], etc. Furthermore, this review is a concerted effort to highlight design, synthetic strategies as well as biological activities of each class of this condensed heterocycle. Structure-activity relationship studies and in silico approaches wherever reported have also been discussed. In addition, manuscript also offers scope for design, synthesis and generation of libraries of unreported classes of pyrazoloquinazolines for the biological evaluation. Copyright ? 2014 Elsevier Masson SAS. All rights reserved.
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    Microwave-assisted synthesis of pyrazolo[1,5-c]quinazolines and their derivatives
    (Elsevier, 2014) Kumar, Deependra; Kumar, Raj
    Microwave accelerated and expedited cyclocondensation reactions of 2-(3-aryl-1H-pyrazol-5-yl)anilines (4) with diverse aryl aldehydes/triethyl orthoformate in water/MeCN (route D) and internal cyclocondensation and aromatization of 5-(2-aminophenyl)-4,5-dihydro-3-arylpyrazole-1-carbaldehyde (7) under MeOH (route E) for the synthesis of a series of pyrazolo[1,5-c]quinazolines and their derivatives (1a–1q) are reported.
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    Design, microwave-mediated synthesis and biological evaluation of novel 4 aryl(alkyl)amino-3-nitroquinoline and 2,4-diaryl(dialkyl) amino-3-nitroquinolines as anticancer agents
    (Elsevier, 2015) Chauhan, Monika; Rana, Anil; Alex, Jimi Marin; Negi, Arvind; Singh, Sandeep; Kumar, Raj
    Design, microwave-assisted synthesis of novel 4-aryl (alkyl)amino-3-nitroquinoline (1a–1l) and 2,4-diaryl (dialkyl)amino-3-nitroquinolines (2a–2k and 3a) via regioselective and complete nucleophilic substitution of 2,4-dichloro-3-nitroquinoline, respectively in water are presented. The newly synthesized compounds were evaluated for the first time for antiproliferative activity against EGFR overexpressing human lung (A-549 and H-460) and colon (HCT-116-wild type and HCT-116-p53 null) cancer cell lines. Some notions about structure–activity relationships (SAR) are presented. Compounds 2e, 2f, 2j and 3a overall exhibited excellent anticancer activity comparable to erlotinib which was used as a positive control. Molecular modeling studies disclosed the recognition pattern of the compounds and also supported the observed SAR.