Pharmaceutical Sciences and Natural Products - Research Publications

Permanent URI for this collectionhttps://kr.cup.edu.in/handle/32116/56

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Subject: search.filters.subject.Indole

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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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    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.