313673-23-3Relevant academic research and scientific papers
ANTIDEPRESSANT HETEROARYL DERIVATIVES OF HETEROCYCLE-FUSED BENZODIOXANS
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Page/Page column 100, (2009/01/24)
The invention provides compounds of the Formula: (I) that are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre- menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa, bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses. The compounds are able to block the recptake of serotonin and are modulators at brain 5HT1A serotonin receptors.
Design, synthesis, and biological evaluation of combretastatin nitrogen-containing derivatives as inhibitors of tubulin assembly and vascular disrupting agents
Monk, Keith A.,Siles, Rogelio,Hadimani, Mallinath B.,Mugabe, Benon E.,Ackley, J. Freeland,Studerus, Scott W.,Edvardsen, Klaus,Trawick, Mary Lynn,Garner, Charles M.,Rhodes, Monte R.,Pettit, George R.,Pinney, Kevin G.
, p. 3231 - 3244 (2007/10/03)
A series of analogs with nitro or serinamide substituents at the C-2′-, C-5′-, or C-6′-position of the combretastatin A-4 (CA4) B-ring was synthesized and evaluated for cytotoxic effects against heart endothelioma cells, blood flow reduction to tumors in
Method for preparing Combretastatin
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Page/Page column 10, (2008/06/13)
The invention concerns novel methods for preparing Combretastatin by Wittig condensation between nitromethoxy-benzaldehyde and a trimethoxybenzyl phosphonium salt or inversely a nitromethoxybenzyl phosphonium salt with trimethoxybenzylaldehyde or further by a Wittig reaction on the same derivatives whereof the nitro function has been reduced into an amino group.
Process for the preparation of combretastatins
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, (2008/06/13)
The present invention provides novel processes for the preparation of combretastatins or stilbene compounds of formulae (I) and (III) wherein A is NH2 or and PG is a protecting group. The disclosed and claimed processes include (1) Wittig condensation between a nitromethoxybenzaldehyde and a trimethoxybenzylphosphonium salt or between a trimethoxybenzaldehyde and a nitromethoxybenzylphosphonium salt to provide an intermediate compound of formula (I) wherein A is NO2, and subsequent iron powder reduction to provide a compound of formula (I) wherein A is NH2; (2) Wittig condensation of the same precursor aldehydes and phosphonium salts wherein NO2 is replaced by NH2 to provide a compound of formula (I) wherein A is NH2; and (3) a process for condensation of a compound of formula (I) wherein A is NH2 with a doubly protected serinamide to provide an intermediate of formula (III), and subsequent hydrolysis to provide a compound of formula (I) wherein A is —NH—C(═O)CH(NH2)CH2OH, or the pharmaceutically acceptable salts thereof. Also claimed is a compound of formula (III).
Synthesis and biological evaluation of aryl azide derivatives of combretastatin a-4 as molecular probes for tubulin
Pinney, Kevin G.,Mejia, Maria P.,Villalobos, Victor M.,Rosenquist, Brent E.,Pettit, George R.,Verdier-Pinard, Pascal,Hamel, Ernest
, p. 2417 - 2425 (2007/10/03)
Two new aryl azides, (Z)-1-(3'-azido-4'-methoxyphenyl)-2-(3'',4'',5''-trimethoxyphenyl)ethene 9 and (Z)-1-(4'-azido-3'-methoxyphenyl)-2-(3'',4'',5''-trimethoxyphenyl)ethene 5, modeled after the potent antitumor, antimitotic agent combretastatin A-4 (CA-4)
