- Synthesis and biological evaluation of novel bavachinin analogs as anticancer agents
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A library of 28 analogs of bavachinin including aliphatic and aromatic ethers, epoxide, chalcone, oxime, semicarbazide, oxime ether and triazole derivatives have been synthesized and evaluated for cytotoxicity against four different human cancer cell lines. Bio-evaluation studies exhibited better cytotoxic profile for many analogs compare to bavachinin. Best results were observed for a 1,2,3-triazole analog (17i) with IC50 values 7.72, 16.08, 7.13 and 11.67 μM against lung (A549), prostate (PC-3), colon (HCT-116) and breast (MCF-7) cancer cell lines respectively. This analog showed three and four fold improvement in cytotoxicity against HCT-116 and A549 cell lines than parent molecule (1). Structure activity relationship (SAR) study for all synthesized analogs was carried out. Further, mechanistic study of the lead molecule (17i) revealed that it inhibits colony formation and in vitro migration of human colon cancer cells (HCT-116). Also, it induced the morphological changes and mediated the apoptotic cell death of HCT-116 cells with perturbance in mitochondrial membrane potential (MMP) and PARP cleavage.
- Gupta, Nidhi,Qayum, Arem,Raina, Arun,Shankar, Ravi,Gairola, Sumeet,Singh, Shashank,Sangwan, Payare L.
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- Synthesis and antibacterial activity of chalcones bearing prenyl or geranyl groups from Angelica keiskei
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Chalcones bearing prenyl or geranyl groups from Angelica keiskei, such as 4-hydroxyderricin (1a), xanthoangelol (1e), xanthoangelol F (1f), xanthoangelol H (2), deoxyxanthoangelol H (3), and deoxydihydroxanthoangelol H (4) and their derivatives were synthesized. From the evaluation of antibacterial activity of the synthesized chalcones, 1a, isobavachalcone (1b), 1e, 1f, bavachalcone (5a), and broussochalcone B (5b) were found to inhibit Gram-positive bacteria.
- Sugamoto, Kazuhiro,Matsusita, Yoh-Ichi,Matsui, Kana,Kurogi, Chiaki,Matsui, Takanao
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p. 5346 - 5359
(2011/08/04)
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- THERAPEUTIC AGENT
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A therapeutic agent and prophylactic agent for a disease accompanying an abnormality in an amount of insulin or insulin response, an agent for an insulin-mimetic action, a food, beverage and feed, an agent for enhancing glucose uptake into a cell, and an agent for inducing differentiation into an adipocyte, characterized in that each comprises as an effective ingredient at least one compound selected from the group consisting of a chalcone compound, an acetophenone compound, a coumarin compound, a phthalide compound, derivatives thereof, and pharmacologically acceptable salts thereof.
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Page/Page column 59
(2010/11/08)
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- An Improved Procedure for Cyclisation of Chalcones to Flavanones Using Celite Supported Potassium Fluoride in Methanol: Total Synthesis of Bavachinin
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Chalcones may be cyclised to the corresponding flavanones by stirring with KF - celite suspended in methanol at reflux.This method gives consistently higher conversion than other reported procedures and its utility is illustrated by the synthesis of the l
- Harwood, Laurence M.,Loftus, Gabriel C.,Oxford, Anona,Thomson, Colin
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p. 649 - 657
(2007/10/02)
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