156812-50-9Relevant academic research and scientific papers
Sulfonamide chalcone as a new class of α-glucosidase inhibitors
Seo, Woo Duck,Kim, Jin Hyo,Kang, Jae Eun,Ryu, Hyung Won,Curtis-Long, Marcus J.,Lee, Hyun Sun,Yang, Min Suk,Park, Ki Hun
, p. 5514 - 5516 (2005)
Chalcones 1-20, a new class of glycosidase inhibitors, were synthesized, and their glycosidase inhibitory activities were investigated. Non-aminochalcones 1-12 had no inhibitory activity, however, aminochalcones 13-20 had strong glycosidase (α-glucosidase, α-amylase, and β-amylase) inhibitory activities. In particular, sulfonamide chalcones 17-20 had more potent α-glucosidase inhibitory activity than aminated chalcone 13-16. 4′-(p-Toluenesulfonamide)-3,4-dihydroxy chalcone 20 (IC50 = 0.4 μM) was the best inhibitor against α-glucosidase, and these sulfonamide chalcones showed non-competitive inhibition.
Design, synthesis, and in vitro evaluation of cytotoxic activity of new substituted 1,4-benzoquinones and hydroquinones
Chaaban, Ibrahim,El-Khawass, El-Sayeda,Mahran, Mona,El-Sayed, Ola,El-Saidi, Hassan,Aboul-Enen, Hassan
, p. 49 - 77 (2008/12/21)
A new series of p-benzoquinones, hydroquinones, and quinol dimethyl ethers substituted by a pyrazole ring either directly or after an oxoethyl linker was synthesized and screened for in vitro cytotoxic activity. Compounds 8d, f, g, i, and 9c, f, and 13c exhibited broad-spectrum activity (GI50 MG-MID values 9.27-14.72 μM). With regard to sensitivity, compounds 8f and 9c, f have proved to possess a remarkable activity against leukemia tumor cell lines (GI50 = 3.43-5.03 μM). Indeed, compound 13c showed the highest activity profile against individual leukemia subpanel cell line SR (GI 50 = 0.91 μM).
Biologically active 1,3-bis-aromatic-prop-2-en-1-ones, 1,3-bis-aromatic-propan-1-ones, and 1,3-bis-aromatic-prop-2-yn-1-ones
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, (2008/06/13)
The invention relates to the use of 1,3-bis-aromatic-prop-2-en-1-ones (chalcones), 1,3-bis-aromatic-propan-1-ones (dihydrochalcones), and 1,3-bis-aromatic-prop-2-yn-1-ones for the preparation of pharmaceutical compositions for the treatment or prophylaxis of a number of serious diseases including i) conditions relating to harmful effects of inflammatory cytokines, ii) conditions involving infection by Helicobacter species, iii) conditions involving infection by viruses, iv) neoplastic disorders, and v) conditions caused by microorganisms or parasites. The invention also relates to novel chalcones and dihydrochalcones (especially alkoxy substituted variants) having advantageous substitution patterns with respect to their effect as drug substances, and to methods of preparing them, as well as to pharmaceutical compositions comprising the novel chalcones. Moreover, the present invention relates to a method for the isolation of Leishmania fumarate reductase, QSAR methodologies for selecting potent compounds for the above-mentioned purposes.
Anti-candida activity of synthetic hydroxychalcones
Tsuchiya,Sato,Akagiri,Takagi,Tanaka,Iinuma
, p. 756 - 758 (2007/10/02)
The antifungal activity of different synthetic hydroxychalcones was determined against Candida species. It was revealed that the presence of hydroxyl groups at C-2, C-4, and C-2' in chalcone was essential to inhibit Candida growth. Among the chalcone derivatives examined, 2,4,2'-trihydroxy-5'-methylchalcone showed the most intensive anti-Candida activity, suggesting that it could be a potential therapeutic agent for candidosis.
