Synthesis and biological evaluation of botulinum neurotoxin a protease inhibitors
NSC 240898 was previously identified as a botulinum neurotoxin A light chain (BoNT/A LC) endopeptidase inhibitor by screening the National Cancer Institute Open Repository diversity set. Two types of analogues have been synthesized and shown to inhibit Bo
Li, Bing,Pai, Ramdas,Cardinale, Steven C.,Butler, Michelle M.,Peet, Norton P.,Moir, Donald T.,Bavari, Sina,Bowlin, Terry L.
experimental part
p. 2264 - 2276
(2010/08/19)
Bisamidine compounds as antiproliferative agents
Known bisamidine compounds are newly discovered to possess DNA methyltransferase inhibiting properties, making them useful for preparing pharmaceutical compositions useful as antiproliferative agents for treating a neoplastic or a non-neoplastic disease characterized by abnormally rapid proliferation of tissue involved in said disease; wherein said bisamidines comprise a compound of Formula (5.0.0): and a pharmaceutically acceptable salt thereof, wherein: —X is —C(R34)—; or —N—; —R23, R24, R28and R29are each independently —H; or —CH2— where R23and R24and R28and R29are taken together with the nitrogen atoms to which they are attached, to form an imidazolinyl group; and —R34is —H; or —CH3. A preferred species of Formula (5.0.0) is the following: 2-(4-Carbamimidoyl-phenyl)-1H-indole-6-carboxamidine.
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(2008/06/13)
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