Application of 52287-51-1. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 6-Bromo-2,3-dihydrobenzo[b][1,4]dioxine, is researched, Molecular C8H7BrO2, CAS is 52287-51-1, about Synthesis and structure-activity relationships of new antiproliferative and proapoptotic retinoid-related biphenyl-4-yl-acrylic acids. Author is Cincinelli, Raffaella; Dallavalle, Sabrina; Nannei, Raffaella; Merlini, Lucio; Penco, Sergio; Giannini, Giuseppe; Pisano, Claudio; Vesci, Loredana; Ferrara, Fabiana Fosca; Zuco, Valentina; Zanchi, Chiara; Zunino, Franco.
Atypical retinoids, or retinoid-related mols. (RRMs), represent a class of proapoptotic agents with a promising potential in the treatment of neoplastic diseases. In the present work, the synthesis and structure-activity relationship of a series of 3′-adamantan-1-yl-biphenyl-4-yl-acrylic acids substituted in ring A were studied. The synthesized compounds were evaluated for their antiproliferative activity in a human promyelocytic leukemia cell line (NB4), and in an ovarian carcinoma cell system including IGROV-1, carrying a functional wild-type p53, and a cisplatin-resistant subline, IGROV-1/Pt-1. The presence of at least one oxygenated substituent in positions 4′ or 5′ appears determinant for the antiproliferative activity. With two substituents of this kind the activity increases, particularly in the case of alkylenedioxy compounds The activation of DNA damage response as indicated by phosphorylation of H2AX histone, RPA-2 protein, and p53 at serine 15 by the most apoptotic compounds provides addnl. support to the hypothesis that the genotoxic stress is a critical event mediating apoptosis induction by compounds of this group.
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Reference:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics