831222-67-4Relevant articles and documents
Amidobenzothiazoles And Process For The Preparation Thereof
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Sheet 4, (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=
Isoxazole-type derivatives related to combretastatin A-4, synthesis and biological evaluation
Kaffy, Julia,Pontikis, Renee,Carrez, Daniele,Croisy, Alain,Monneret, Claude,Florent, Jean-Claude
, p. 4067 - 4077 (2007/10/03)
Novel combretastatin analogues bearing various five-membered heterocycles with consecutive oxygen and nitrogen atoms, in place of the olefinic bridge of CA4, have been synthesized (isoxazole, isoxazoline, oxadiazole, etc). These compounds have been evalua
Heterocyclic and phenyl double-bond-locked combretastatin analogues possessing potent apoptosis-inducing activity in HL60 and in MDR cell lines
Simoni, Daniele,Grisolia, Giuseppina,Giannini, Giuseppe,Roberti, Marinella,Rondanin, Riccardo,Piccagli, Laura,Baruchello, Riccardo,Rossi, Marcello,Romagnoli, Romeo,Invidiata, Francesco Paolo,Grimaudo, Stefania,Jung, M. Katherine,Hamel, Ernest,Gebbia, Nicola,Crosta, Lucia,Abbadessa, Vincenzo,Di Cristina, Antonietta,Dusonchet, Luisa,Meli, Maria,Tolomeo, Manlio
, p. 723 - 736 (2007/10/03)
Two new series of combretastatin (CA-4) analogues have been prepared. The alkenyl motif of CA-4 was replaced either by a five-membered heterocyclic (isoxazoline or isoxazole) or by a six-membered ring (pyridine or benzene). The new compounds have been evaluated for their effects on tubulin assembly and for cytotoxic and apoptotic activities. Five compounds (18b, 20a, 21a, 34b, and 35b) demonstrated an attractive profile of cytotoxicity (IC50 1 μM) and apoptosis-inducing activity but poor antitubulin activity. The isoxazoline derivatives 18b, 20a, and 21a, demonstrated potent apoptotic activity different from that of natural CA-4. Their ability to block most cells in the G2 phase suggests that these compounds could act on targets different from the mitotic spindle. This would indicate activation of both the intrinsic and the extrinsic apoptotic pathways. The data suggest unambiguously that structural alteration of the stilbene motif of CA-4 can be extremely effective in producing potent apoptosis-inducing agents.
COMBRETASTATIN DERIVATIVES WITH CYTOTOXIC ACTION
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Page 21; 22, (2010/02/10)
The invention described herein relates to new combretastatin derivatives obtained by total synthesis and having the following general formula (I) in which the groups are as defined in the description here below. Said compounds, though chemically related to the structure of cis/trans-combretastatin, do not always bind tubulin, but nevertheless exhibit cytotoxic activity of interest in the oncological field as anticancer and/or antiangiogenic agents.