School Of Basic And Applied Sciences

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Subject: search.filters.subject.Chromene

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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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    Gaussian field-based comparative 3D QSAR modelling for the identification of favourable pharmacophoric features of chromene derivatives as selective inhibitors of ALR2 over ALR1
    (Springer, 2021-01-07T00:00:00) Verma, Sant Kumar; Kumar, Niraj; Thareja, Suresh
    Aldehyde reductase (ALR1) and aldose reductase (ALR2) are both oxo-reductase enzymes of aldo-keto reductase (AKR) superfamily involved in several cellular processes. ALR1 plays an important role in colorectal cancer, lungs, and hepatic carcinoma, while ALR2 is involved in diabetic complications like retinopathy, neuropathy, and nephropathy cataract. Both the enzymes take part in distinct physiological processes, however, share more > 70% structural homology. This is the major cause behind the unachieved target selectivity of molecules that entered the development pipeline as ALR2 inhibitors. Chromene analogues have been widely explored for diverse biological activities, including antioxidant and diabetic complication prevention potential. For the identification of spatial fingerprints of target-specific chromene bearing ALR2 inhibitors over ALR1, Gaussian field-based comparative 3D QSAR models were generated on a dataset having ALR1 and ALR2 inhibitory activity. Both the ALR1 and ALR2 3D QSAR models were statistically fit with good predictive ability concerning PLS generated validation constraints. The comparative steric, electrostatic, hydrophobic, HBA, and HBD features were elucidated using respective contour maps for selective target specific favourable activity against ALR2 over ALR1. In addition, the five-point pharmacophores for ALR1 and ALR2 favourable features were also generated using the DHHRR_1 hypothesis for better insight on the distinctive features of ALR2 inhibitors compared to ALR1. � 2021, The Author(s), under exclusive licence to Springer Science+Business Media, LLC part of Springer Nature.
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    Identification of novel indole based heterocycles as selective estrogen receptor modulator.
    (Elsevier, 2018) Singla, Ramit; Prakash, Kunal; Gupta Kunj Bihari; Upadhyay, Shishir; Dhiman, Monisha; Jaitak, Vikas
    In the present study, we have designed and synthesized indole derivatives by coalescing the indole nucleus with chromene carbonitrile and dihydropyridine nucleus. Two compounds 5c and 6d were selected from series I and II after sequential combinatorial library generation, docking, absorption, distribution, metabolism and excretion (ADME) filtering, anti-proliferative activity, cytotoxicity, and ER-α competitor assay kit by utilizing estrogen receptor-α (ER-α) dominant T47D BC cells line and PBMCs (Peripheral Blood Mononuclear Cells). Cell imaging experiment suggested that both the compounds successfully cross cellular biomembrane and accumulate in nuclear, cytoplasmic and plasma membrane region. Semiquantitative RT-PCR and Western blotting experiments further supported that both compounds reduced the expression of mRNA and receptor protein of ER-α, thereby preventing downstream transactivation and signaling pathway in T47D cells line. Current findings imply that 5cand 6d represent novel ER-α antagonists and may be used in the development of chemotherapy for the management of BC.