19479-83-5Relevant articles and documents
Design, synthesis, and biological evaluation of a novel series of bisintercalating DNA-binding piperazine-linked bisanthrapyrazole compounds as anticancer agents
Zhang, Rui,Wu, Xing,Yalowich, Jack C.,Hasinoff, Brian B.
, p. 7023 - 7032 (2011)
A series of bisintercalating DNA binding bisanthrapyrazole compounds containing piperazine linkers were designed by molecular modeling and docking techniques. Because the anthrapyrazoles are not quinones they are unable to be reductively activated like doxorubicin and other anthracyclines and thus they should not be cardiotoxic. The concentration dependent increase in DNA melting temperature was used to determine the strength of DNA binding and the bisintercalation potential of the compounds. Compounds with more than a three-carbon linker that could span four DNA base pairs achieved bisintercalation. All of the bisanthrapyrazoles inhibited human erythroleukemic K562 cell growth in the low to submicromolar concentration range. They also strongly inhibited the decatenation activity of topoisomerase IIα and the relaxation activity of topoisomerase I. However, as measured by their ability to induce double strand breaks in plasmid DNA, the bisanthrapyrazole compounds did not act as topoisomerase IIα poisons. In conclusion, a novel group of bisanthrapyrazole compounds were designed, synthesized, and biologically evaluated as potential anticancer agents.
PROCESS FOR MANUFACTURING ALKYLENEAMINE COMPOUNDS
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Page/Page column 19, (2020/08/22)
The invention pertains to a process for manufacturing alkyleneamine compounds, comprising the steps of - in a reaction medium reacting an alkyleneurea compound comprising at least one primary amine group, or at least one cyclic secondary amine group, or at least one primary amine group and at least one cyclic secondary amine group, and at least one cyclic alkyleneurea group of formula I wherein A is selected from the group of C2 to C4 alkylene units, optionally substituted by one or more C1 to C3 alkyl groups, with an alkylhalide compound to form an alkyleneamine hydrohalide salt comprising at least one cyclic alkyleneurea group of formula I, the alkylhalide compound being selected from the group of haloalkanes with 2-6 halogen atoms, and haloaminoalkanes, and - reacting the alkyleneamine hydrohalide salt with a base to form an alkyleneamine compound comprising at least one cyclic alkyleneurea group of formula I. In one embodiment the reaction is carried out in the presence of one or more of ammonia and additional alkyleneamine compound. The process according to the invention produces less cyclic and branched side products and more straight-chain higher alkyleneamines than conventional processes, in particular more straight-chain ethyleneamines selected from L-TETA, L-TEPA, and L-PEHA.
BIS-DIAZENIUMDIOLATE COMPOUNDS AS ANTI-CANCER AGENTS
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Paragraph 0040; 0041; 0048, (2019/04/25)
A series of double-component, bis O2-aryl diazeniumdiolate derivatives are provided, of which each molecule can release up to four nitric oxide molecules. These compounds show cytotoxic activities to cancer cells, such as human leukemia, breast cancer and lung cancer. Among them, the compound 3 showed the highest specific activity against human leukemia cells.
