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In the current scenario, development of anticancer drugs with specific targets is of prime importance in modern chemical biology. Observing the importance of benzophenone and coumarin nucleus, it would be worthwhile to design and synthesize novel benzophenone derivatives (8a-o) bearing the coumarin nucleus. Further, they were screened for prospective anticancer activities in vitro against the Michigan Cancer Foundation-7 (MCF-7) and Ehrlich's ascites tumor (EAT) cell lines and their biomarkers, followed by in silico studies regarding phosphoinositide 3-kinase (PI3K) and caspase by molecular docking. Benzophenones have been reported as potential drugs targeting tumor angiogenesis; thus, the formation of neovessels in an in vivo model system like CAM, which is angiogenesis dependent, was observed in the presence of compounds 8a-o. The above findings would help in understanding their putative potential as therapeutic agents for cancer patients.

In building upon the increasing utility of avian immunology as an alternative to the use of mammalian systems for assessing immunotoxic potentials of environmentally and/or occupationally encountered chemicals, in vitro studies were performed to determine if easily obtainable freshly harvested cells from White Leghorn chickens could be used to detect effects on a critical immune cell type by any given toxicant. These studies also sought to determine if these cells could also potentially provide a vehicle to elucidate potential mechanisms underlying effects previously described for the test agent in in vivo investigations. Here, specifically, the toxic effect (and thus, ultimately, the potential to be an immunotoxicant in situ) of a commonly used commercially available form of deltamethrin on Leghorn lymphocytes was examined. The toxicity of this synthetic pyrethroid was evaluated by assaying both lymphoproliferation and apoptosis after exposure. A significant (p < 0.05) inhibitory effect of deltamethrin on mitogen-stimulated lymphocytes was observed at 10(- 5) M. Apoptosis was detected using DNA ladder analyses; annexin-V binding assays incorporating an immunoperoxidase technique were used to identify translocated phosphatidylserine; and, electron microscopy, including both scanning and transmission types, were used to detect ultrastructural changes (e.g., chromatin condensation, membrane blebbing and phagocytosis) in deltamethrin-treated cells. Our results indicated that deltamethrin, even at a very low dose, could give rise to potential immunotoxicities in situ by inducing toxicity (i.e., apoptosis) in immunogenic cells. Our results also show that this particular in vitro system may be used as an alternative to standard laboratory animals for the performance of immunotoxicity experiments involving pesticides.

Design, Synthesis, and Anticancer Properties of Novel Benzophenone-Conjugated Coumarin Analogues. -Compounds (Ic)-(Ie) show potent anticancer activity against MCF-7 cells. -(RANGANATHA, V. L.; ZAMEER, F.; MEGHASHRI, S.; REKHA, N. D.; GIRISH, V.; GURUPADASWAMY, H. D.; KHANUM*, S. A.; Arch. Pharm. (Weinheim, Ger.) 346 (2013) 12, 901-911, http://dx.doi.org/10.1002/ardp.201300298 ; Dep. Chem., Yuvaraja Coll., Univ. Mysore, Mysore 570 005, India; Eng.) -H. Toeppel

The increasing prevalence of gout has been accompanied by a growing number of patients intolerant to or with disease refractory to the available urate-lowering therapies. This metabolic disease is a common disease with a higher prevalence in men older than 30 years and in women older than 50 years. These findings highlight the need for emerging treatments to effectively lower urate levels. In this view, we describe the xanthine oxidase (XO) inhibitory activities of the synthesized compounds 5a-j and also their antioxidant activities. Compounds 5c, 5d, 5f, 5h, and 5j exhibited good inhibitory activities against XO. On the other hand, compounds 5g and 5j exhibited moderate antioxidant activity.

Title compounds (V) exhibit good inhibitory activities against xanthine oxidase.