97315-19-0Relevant academic research and scientific papers
Amidobenzothiazoles And Process For The Preparation Thereof
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, (2013/12/04)
The present invention provides a compound of general formulae A useful as potential anti-cancer agents against human cancer cell lines and a process for the preparation thereof. Where in R, R1, R2═H, alkyl, alkoxy, halo, haloalkyl, halomethoxy, nitro and G= Where in R, R1, R2═H, alkyl, alkoxy, halo, haloalkyl, halomethoxy, nitro and G=
1,2,3-Triazole analogs of combretastatin A-4 as potential microtubule-binding agents
Odlo, Kristin,Fournier-Dit-Chabert, Jérémie,Ducki, Sylvie,Gani, Osman A.B.S.M.,Sylte, Ingebrigt,Hansen, Trond Vidar
experimental part, p. 6874 - 6885 (2010/10/19)
A series of cis-restricted 1,4- and 1,5-disubstituted 1,2,3-triazole analogs of combretastatin A-4 (1) have been prepared. Cytotoxicity and tubulin inhibition studies showed that 2-methoxy-5-((5-(3,4,5-trimethoxyphenyl)-1H-1,2, 3-triazol-1-yl)methyl)aniline (5e) and 2-methoxy-5-(1-(3,4,5-trimethoxybenzyl)- 1H-1,2,3-triazol-5-yl)aniline (6e) were two of the most active compounds. Molecular modeling studies revealed that the N-2 and N-3 atoms in the triazole rings in 5e and 6e did not form hydrogen bonds with the amino acids in the anticipated pharmacophore.
PROCESSES FOR PREPARING (E)-STYRYLBENZYLSULFONE COMPOUNDS AND USES THEREOF FOR TREATING PROLIFERATIVE DISORDERS
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Page/Page column 28, (2010/06/22)
Processes for preparing (E)-2,4,6-(Trimethoxystyryl)-3-O-Phosphate Disodium-4-Methoxybenzyl Sulfones and uses thereof as antiproliferative agents, including, for example, anticancer agents, and as radioprotective and chemoprotective agents.
Substituted Phenoxy-and Phenylthio-Derivatives for Treating Proliferative Disorders
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, (2010/11/30)
Substituted phenol derivatives of Formula (I) are useful as antiproliferative agents including, for example, anticancer agents, and as radioprotective and chemoprotective agents.
Design, synthesis, and biological evaluation of (E)-styrylbenzylsulfones as novel anticancer agents
Reddy, M. V. Ramana,Mallireddigari, Muralidhar R.,Cosenza, Stephen C.,Pallela, Venkat R.,Iqbal, Nabisa M.,Robell, Kimberly A.,Kang, Anthony D.,Reddy, E. Premkumar
, p. 86 - 100 (2008/09/20)
Cell cycle progression is regulated by cyclins and cyclin-dependent kinases, which are formed at specific stages of the cell cycle and regulate the G1/S and G2/M phase transitions, employing a series of "checkpoints" governed by phosphorylation of their substrates. Tumor development is associated with the loss of these checkpoint controls, and this provides an approach for the development of therapeutic agents that can specifically target tumor cells. Here, we describe the synthesis and SAR of a novel group of cytotoxic molecules that selectively induce growth arrest of normal cells in the G1 phase while inducing a mitotic arrest of tumor cells resulting in selective killing of tumor cell populations with little or no effect on normal cell viability. The broad spectrum of antitumor activity in vitro and xenograft models, lack of in vivo toxicity, and drug resistance suggest potential for use of these agents in cancer therapy.
ACTIVATED CYTOTOXIC COMPOUNDS FOR ATTACHMENT TO TARGETING MOLECULES FOR THE TREATMENT OF MAMMALIAN DISEASE CONDITIONS
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Page/Page column 55, (2010/11/30)
Activated cytotoxic compounds are described for attachment to targeting molecules for the treatment of a mammalian disease condition which comprise, an activator, a spacer linker, a linker (e.g., self-immolative), and a cytotoxic drug selected from the group consisting of AMINO-SUBSTITUTED (E)-2,6-DIALKOXYSTYRYL 4-SUBSTITUTED BENZYLSULFONES, AMINO-AND- HYDROXY SUBSTITUTED STYRYLSULFONANILIDES, and SUBSTITUTED PHENOXY- AND PHENYLTHIO-STYRYLSULFONE DERIVATIVES. Activated cytotoxic compound attached to a targeting molecule are described wherein the targeting molecule is selected from the group consisting essentially of an antibody, a receptor, a ligand, a cytokine, a hormone, and a signal transduction molecule. The invention is further directed to a method of treatment of disease conditions.
COMPOSITION AND METHODS FOR THE TREATMENT OF PROLIFERATIVE DISEASES
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Page/Page column 35-36, (2010/11/24)
Methods and compositions are provided for treating proliferative disorders, wherein the composition comprises at least one compound according to Formula (I), wherein R1 is selected from the group consisting of -OH, -NH2, -NH-CH2
