1334138-00-9Relevant articles and documents
Accessing Polyoxygenated Dibenzofurans via the Union of Phenols and o-Benzoquinones: Rapid Syntheses of Metabolites Isolated from Ribes takare
Zhang, Meng Yao,Barrow, Russell A.
, p. 2302 - 2305 (2017)
The construction of polyoxygenated dibenzo[b,d]furan frameworks from the union of substituted phenols/naphthols and o-benzoquinones via a Michael-oxidation-oxa-Michael cascade is reported. The power of this transformation is demonstrated in the generation of a library of highly substituted dibenzofurans, featuring specifically substituted molecules containing broad ranges of functionality. The utility of this method is showcased in the total syntheses of two dibenzofurans isolated from Ribes takare, assembling the carbon scaffold of both natural products in one operation.
Synthesis of aryl-substituted naphthalene-linked pyrrolobenzodiazepine conjugates as potential anticancer agents with apoptosis-inducing ability
Kamal, Ahmed,Reddy, M. Kashi,Ramaiah, M. Janaki,Srikanth,Rajender,Reddy, V. Santosh,Kumar, G. Bharath,Pushpavalli,Bag, Indira,Juvekar, Aarti,Sen, Subrata,Zingde, Surekha M.,Pal-Bhadra, Manika
experimental part, p. 1665 - 1679 (2012/01/05)
A library of new aryl-substituted naphthalene C8-linked pyrrolo[2,1-c][1,4]benzodiazepine (PBD) conjugates with various linker architectures were designed, synthesized, and evaluated for their anticancer activity against a panel of 11 human cancer cell lines. All 32 conjugates show anticancer potential, with some of them exhibiting particularly high activity (0.01-0.19μM). Thermal denaturation studies showed effective DNA binding capacity relative to DC-81. In assays for biological activity relating to cell-cycle distribution, these PBD conjugates induce G0/G1-phase arrest and also cause an increase in the levels of p53 and caspase-9 proteins, followed by apoptotic cell death. One conjugate in particular is the most promising candidate of the series, with the potential to be selected for further studies, either alone or in combination with existing anticancer therapies. Getting into the groove: Pyrrolobenzodiazepine (PBD) conjugates showed an effective ability to bind DNA. They induce G0/G1-phase arrest, enhance the expression levels of p53 and caspase-9, and induce apoptosis. One conjugate stands out as particularly promising; it is a suitable candidate for further study, either alone or in combination with current anticancer therapies.