School Of Basic And Applied Sciences

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Subject: search.filters.subject.Indole

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Now showing 1 - 6 of 6
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    Recent development in indole derivatives as anticancer agent: A mechanistic approach
    (Bentham Science Publishers, 2021-01-05T00:00:00) Devi, Neha; Kaur, Kamalpreet; Biharee, Avadh; Jaitak, Vikas
    Background: Cancer accounts for several deaths each year. There are multiple FDA approved drugs for cancer treatments. Due to the severe side effects and multiple drug resistance, the current drug therapies become ineffective. So, the newer moieties with fewer toxic effects are necessary for the development. Objective: The mechanism of indole derivatives as anti-cancer agents with their major target is explored in detail in this article. Methods: Recent advances and mechanism of indole derivatives as anti-cancer agents are reviewed. This review suggests a detailed explanation of multiple mechanisms of action of various indole derivatives: cell cycle arrest, aromatase inhibitor estrogen receptor regulator, tubulin inhibitor, a tyrosine kinase inhibitor, topoisomerase inhibitors, and NFkB/PI3/Akt/mTOR pathway inhibitors, through which these derivatives have shown promising anti-cancer potential. Results: A full literature review showed that the indole derivatives are associated with the properties of inducing apoptosis, aromatase inhibition, regulation of estrogen receptor and inhibition of tyrosine kinase, tubulin assembly, NFkB/PI3/Akt/mTOR pathway, and HDACs. These derivatives have shown significant activity against cancer cell lines. Conclusion: Indole derivatives seem to be important in cancer via acting through various mechanisms. This review has shown that the indole derivatives can further be explored for the betterment of cancer treatment, and to discover the hidden potential of indole derivatives. � 2021 Bentham Science Publishers.
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    Naturally available nitrogen-containing fused heterocyclics as prospective lead molecules in medicinal chemistry
    (Bentham Science Publishers, 2020-02-17T00:00:00) Bhardwaj, Nivedita; Pathania, Akashdeep; Kumar, Pradeep
    Heterocyclic compounds constitute one of the largest and most versatile families of organic compounds. There are many heterocyclic compounds that are being isolated from natural sources and day by day the number is increasing rapidly due to their enormous utili-ty. Nitrogen containing heterocyclic compounds have a prominent role in medicinal chemis-try, biochemistry and other streams of science. In this review, we have covered most of the biologically active nitrogen containing heterocyclic compounds obtained from the natural sources including indole, carbazole, quinoline, isoquinoline and benzothiazole ring system. These isolated nitrogen containing heterocyclic compounds render wide spectrum of biological activities including antifungal, anti-inflammatory, antibacterial, antioxidants, anticonvul-sant, anti-allergic, herbicidal and anticancer activities. � 2021 Bentham Science Publishers.
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    Chitosan-supported FeCl3 catalyzed multicomponent synthesis of tetrahydroisoquinoline-indole hybrids with promising activity against chloroquine resistant Plasmodium falciparum
    (Elsevier B.V., 2022-10-26T00:00:00) Kaur, Pavneet; Sharma, Priyanka; Kumar, Vinod; Sahal, Dinkar; Kumar, Rakesh
    An operationally simple three-component coupling of tetrahydroisoquinoline (THIQ), aldehydes and indoles or indole-3-carboxylic acids has been achieved using chitosan-ionic liquid supported FeCl3 (chit-IL@FeCl3) as a recyclable heterogeneous catalyst. The developed waste-free approach provided rapid access to biologically important THIQ-indole hybrids without the use of any additive or ligand. The synthesized THIQ-indole hybrids were evaluated as antiplasmodial agents against chloroquine-sensitive (Pf3D7) and chloroquine-resistant (PfINDO) strains of Plasmodium falciparum. Compounds 4b (most potent against Pf3D7) and 4g (most potent against PfINDO) showed IC50 values of 1.32 and 0.26 �g/mL respectively. Also, 4g showed strong cytocidal action against both rings and trophozoite stages. Furthermore, cytotoxic study against human liver HUH 7 cells revealed that the most potent compound 4g with an excellent resistance index of 0.07 is also relatively non-toxic. The results of this study suggest that THIQ-indole hybrids hold an enormous potential for developing new antimalarial agents with novel mechanism of action. � 2022 Elsevier B.V.
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    Recent advances for construction and late-stage diversification of indole core via C-H bond activation/functionalization
    (Elsevier, 2021-02-26T00:00:00) Sinha, Arun Kumar; Kumar, Rakesh
    Indole is an important structural motif of various drugs, therapeutic leads besides its prevalence in numerous natural products, agrochemicals, perfumery, and dyes. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials. Owing to such a huge potential, continuous efforts are being put forward to construct or diversify this scaffold. This chapter provides an overview of various recently developed methodologies for the construction of indole core via C-H bond activation/functionalization. In particular, Pd- and Ru-mediated cyclization strategies involving Csp2-H functionalization of monofunctionalized arene substrates with the unsaturated bond of alkene and alkyne are highlighted herein. Also, late-stage diversification of indole system (C4-C7 position) via direct C-H activation is covered. Furthermore, the mechanistic aspects of some of these reactions are discussed as well. � 2021 Elsevier Inc. All rights reserved.
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    Identification of Novel Indole Derivatives as Potent ?-Amylase Inhibitors for the Treatment of Type-II Diabetes Using in-Silico Approaches
    (AMG Transcend Association, 2022-04-09T00:00:00) Khatabi, Khalil El; El-Mernissi, Reda; Hajji, Halima; Singh, Atul Kumar; Ajana, Mohammed Aziz; Lakhlifi, Tahar; Kumar, Shashank; Bouachrine, Mohammed
    The ?-amylase is regarded as a promising drug target for diabetes mellitus-type II. Hence, inhibiting ?-amylase activity is a potential drug discovery approach for treating this chronic metabolic disorder. The present study explores the structural requirements and understands the inhibition mechanism of the novel developed indole-based derivatives as ?-amylase inhibitors through 3D-QSAR, molecular docking, ADMET, and molecular dynamics (MD) simulation. The 3D-QSAR study showed good statistical reliability for two developed predictive models; CoMFA and CoMSIA. Through a deep investigation of docking analysis, detailed interactions with ?-amylase of the most active compound 7 were explored. Four new indole derivatives were designed based on the contour maps and docking analysis, with significantly higher inhibitory activity than the molecules in the dataset. The selected molecules were evaluated for pharmacokinetic properties, showing a reasonably good ADMET profile. Furthermore, a 20-ns MD simulation of selected compounds bound to ?-amylase was performed to ensure stability during simulation further. Greater stability of the designed molecule-protein complex A1 was found. The present findings shed light on the binding mode and the interactions between newly designed compounds, especially compound A1 and ?-amylase and may be beneficial for drug development efforts targeting type-II diabetes. � 2022 by the authors.
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    Recent development in indole derivatives as anticancer agents for breast cancer
    (Bentham Science Publishers, 2019) Kaur K.; Jaitak V.
    Background: Breast Cancer (BC) is the second most common cause of cancer related deaths in women. Due to severe side effects and multidrug resistance, current therapies like hormonal therapy, surgery, radiotherapy and chemotherapy become ineffective. Also, the existing drugs for BC treatment are associated with several drawbacks such as poor oral bioavailability, non-selectivity and poor pharmacodynamics properties. Therefore, there is an urgent need for the development of more effective and safer anti BC agents. Objective: This article explored in detail the possibilities of indole-based heterocyclic compounds as anticancer agents with breast cancer as their major target. Methods: Recent literature related to indole derivatives endowed with encouraging anti BC potential is reviewed. With special focus on BC, this review offers a detailed account of multiple mechanisms of action of various indole derivatives: aromatase inhibitor, tubulin inhibitor, microtubule inhibitor, targeting estrogen receptor, DNA-binding mechanism, induction of apoptosis, inhibition of PI3K/AkT/NFkB/mTOR, and HDAC inhibitors, by which these derivatives have shown promising anticancer potential. Results: Exhaustive literature survey indicated that indole derivatives are associated with properties of inducing apoptosis and disturbing tubulin assembly. Indoles are also associated with the inhibition of NFkB/mTOR/PI3K/AkT and regulation of estrogen-mediated activity. Furthermore, indole derivatives have been found to modulate critical targets such as topoisomerase and HDAC. These derivatives have shown significant activity against breast cancer cells. Conclusion: In BC, indole derivatives seem to be quite competent and act through various mechanisms that are well established in case of BC. This review has shown that indole derivatives can further be explored for the betterment of BC chemotherapy. A lot of potential is still hidden which demands to be discovered for upgrading BC chemotherapy.