School Of Basic And Applied Sciences

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    Naturally occurring fused pyrimidine derivatives and their medicinal attributes
    (Elsevier, 2022-10-14T00:00:00) Maity, Pritam; Katiyar, Madhurendra K.; Kumar, Raj
    A wide variety of fused pyrimidine derivatives, mainly occurring as alkaloids, are obtained from different natural sources worldwide. These have been documented to exert some important biological activities including anticancer, antimicrobial, anti-inflammatory, etc. Based on the natural source, these fused pyrimidine derivatives are categorized and discussed further in the subsequent sections highlighting their medicinal attributes. � 2023 Elsevier Ltd. All rights reserved.
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    Naphthylisoindolinone alkaloids: the first ring-contracted naphthylisoquinolines, from the tropical liana Ancistrocladus abbreviatus, with cytotoxic activity
    (Royal Society of Chemistry, 2022-10-12T00:00:00) Fayez, Shaimaa; Bruhn, Torsten; Feineis, Doris; Assi, Laurent Ak�; Kushwaha, Prem Prakash; Kumar, Shashank; Bringmann, Gerhard
    The West African liana Ancistrocladus abbreviatus is a rich source of structurally most diverse naphthylisoquinoline alkaloids. From its roots, a series of four novel representatives, named ancistrobrevolines A-D (14-17) have now been isolated, displaying an unprecedented heterocyclic ring system, where the usual isoquinoline entity is replaced by a ring-contracted isoindolinone part. Their constitutions were elucidated by 1D and 2D NMR and HR-ESI-MS. The absolute configurations at the chiral axis and at the stereogenic center were assigned by using experimental and computational electronic circular dichroism (ECD) investigations and a ruthenium-mediated oxidative degradation, respectively. For the biosynthetic origin of the isoindolinones from �normal� naphthyltetrahydroisoquinolines, a hypothetic pathway is presented. It involves oxidative decarboxylation steps leading to a ring contraction by a benzilic acid rearrangement. Ancistrobrevolines A (14) and B (15) were found to display moderate cytotoxic effects (up to 72%) against MCF-7 breast and A549 lung cancer cells and to reduce the formation of spheroids (mammospheres) in the breast cancer cell line. � 2022 The Royal Society of Chemistry.
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    Steering the antitumor drug discovery campaign towards structurally diverse indolines
    (Academic Press Inc., 2020) Thakur A.; Singh A.; Kaur N.; Ojha R.; Nepali K.
    Indoline framework is often perpended as a privileged heterocycle present in medicinally valuable compounds of natural and synthetic origin. This review article presents the rational approaches/strategies employed for the design of anticancer indolines along with the structure activity relationship and mechanistic insights revealed in the in-vitro and in-vivo assays. The chemist has always been fascinated towards the indoline ring for the construction of antitumor scaffolds owing to its versatility as evidenced by its existence in scaffolds inducing antiproliferative effects via diverse mechanisms. To the delight of medicinal chemist, the applicability of indoline has also been expanded towards the design of dual inhibitors (multitargeting anticancer agents) as well as PROTACS. Overall, it can be concluded that indoline moiety is a magic bullet and the scaffolds containing this ring are foraying towards detailed preclinical and clinical stage investigations by leaps and bounds.
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    Plant-derived natural alkaloids as new antimicrobial and adjuvant agents in existing antimicrobial therapy
    (Bentham Science Publishers, 2019) Pal Mittal R.; Jaitak V.
    Infectious diseases, instigated by pathogenic microorganisms are the cause of numerous health problems in developing countries. Infectious diseases got a place in the list of top ten death causes worldwide. The reason behind that level of severity is antimicrobial resistance. Antimicrobial resistance makes the antimicrobial agents useless when used in the treatment of infectious diseases. Microbes have very smartly achieved resistance against synthetic and semi-synthetic antimicrobial agents for their survival. Therefore, the handling of these diseases has become challenging. The resistance developing power is the reason for their existence since a million years. Due to their highly dangerous nature, proper treatment of infectious diseases has become a topic of concern. This leads the scientists or researchers to focus their research towards natural agents. Plants synthesize secondary metabolites to cope up with biotic and abiotic changes in the environment. Alkaloids are one of the secondary metabolites, synthesized by plants. Alkaloids protect the plant from predators and help them to fight with pathogens. The protecting nature of alkaloids can be used as a strong weapon in battle with resistant microorganisms. The purpose of this review is to provide information about the antimicrobial activity of alkaloids obtained from different plants and their combination with synthetic antimicrobials. Their mechanism of action against microorganisms is also given in the review.