Department Of Pharmaceutical Sciences and Natural Products

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Author: search.filters.author.Alex, Jimi Marin

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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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    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.
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    Pyrimidine-fused derivatives: Synthetic strategies and medicinal attributes
    (Bentham Science Publishers B.V., 2016) Joshi, Gaurav; Nayyar, Himanshu; Alex, Jimi Marin; Vishwakarma, Gajendra S.; Mittal, Sunil; Kumar, Raj
    Pyrimidine-fused derivatives traits the inextricable part of DNA and RNA, exhibit indispensable role in numerous biological processes, possessing momentous chemical and biological importance. Pyrimidine-condensed derivatives as the pharmacophore exhibit broad spectrum of biological activities encompassing antitubercular, antibacterial, antifungal, antiviral, anti-inflammatory, antimalarial, anticancer and anti-HIV. Several retrosynthetic approaches, are available for the synthesis of pyrimidine-fused analogues which offers enormous scope in the field of medicinal chemistry. Ring fused pyrimidine and their innumerable derivatives continue to hold the attention of chemists since their presence in the biologically active resources have been known to elicit additive effects on the bio-efficacy of the molecules. The present review is a concerted effort to congregate information mainly focusing on the comprehensive categorization of pyrimidine ring based on their fusion with five, six, seven and eight-membered ring(s). Moreover, it also puts forward their systematic nomenclature, synthetic strategies, and bioactivities including SAR studies. This review is being put forwarded with an incentive to provide researchers with a comprehensive and updated literature. In addition, the manuscript also brings to light the various pharmacophore designs based on fusedpyrimidine ring system, delving deeper into synthesis and the subsequent generation of new libraries of pyrimidine-fused derivatives including their biological assessments. ? 2016 Bentham Science Publishers.