Developments of combretastatin A-4 derivatives as anticancer agents
YS Shan, J Zhang, Z Liu, M Wang… - Current medicinal …, 2011 - ingentaconnect.com
Tubulin protein is one of several members of a small family of globular proteins. It offers a
potential target for anticancer drug design and development. Combretastatin A-4 (CA-4) is a …
potential target for anticancer drug design and development. Combretastatin A-4 (CA-4) is a …
[HTML][HTML] Microtubule-targeted agents: when mitochondria become essential to chemotherapy
A Rovini, A Savry, D Braguer, M Carré - Biochimica et Biophysica Acta (BBA …, 2011 - Elsevier
Microtubule-Targeting Agents (MTAs) constitute a class of drugs largely used for cancer
treatment in adults and children. In cancer cells, they suppress microtubule dynamics, and …
treatment in adults and children. In cancer cells, they suppress microtubule dynamics, and …
Synthesis, evaluation and structural studies of antiproliferative tubulin-targeting azetidin-2-ones
NM O'Boyle, LM Greene, O Bergin, JB Fichet… - Bioorganic & medicinal …, 2011 - Elsevier
A series of azetidin-2-ones substituted at positions 1, 3 and 4 of the azetidinone ring scaffold
were synthesised and evaluated for antiproliferative, cytotoxic and tubulin-binding activity. In …
were synthesised and evaluated for antiproliferative, cytotoxic and tubulin-binding activity. In …
Design, synthesis, biological evaluation, and structure–activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl) benzenesulfonates as new tubulin …
Sixty-one phenyl 4-(2-oxoimidazolidin-1-yl) benzenesulfonates (PIB-SOs) and 13 of their
tetrahydro-2-oxopyrimidin-1 (2 H)-yl analogues (PPB-SOs) were prepared and biologically …
tetrahydro-2-oxopyrimidin-1 (2 H)-yl analogues (PPB-SOs) were prepared and biologically …
Designing glucokinase activators with reduced hypoglycemia risk: discovery of N, N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl) benzofuran-4-yloxy) …
JA Pfefferkorn, A Guzman-Perez, PJ Oates… - …, 2011 - pubs.rsc.org
Glucokinase is a key regulator of glucose homeostasis and small molecule activators of this
enzyme represent a promising opportunity for the treatment of Type 2 diabetes. Several …
enzyme represent a promising opportunity for the treatment of Type 2 diabetes. Several …
Synthesis, biochemical and molecular modelling studies of antiproliferative azetidinones causing microtubule disruption and mitotic catastrophe
NM O'Boyle, M Carr, LM Greene, NO Keely… - European journal of …, 2011 - Elsevier
The structure-activity relationships of antiproliferative β-lactams, focusing on modifications at
the 4-position of the β-lactam ring, is described. Synthesis of this series of compounds was …
the 4-position of the β-lactam ring, is described. Synthesis of this series of compounds was …
Substituted phenyl 4-(2-oxoimidazolidin-1-yl) benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure …
The importance of the bridge linking the two phenyl moieties of substituted phenyl 4-(2-
oxoimidazolidin-1-yl) benzenesulfonates (PIB-SOs) was assessed using a sulfonamide …
oxoimidazolidin-1-yl) benzenesulfonates (PIB-SOs) was assessed using a sulfonamide …
Novel 3, 4-isoxazolediamides as potent inhibitors of chaperone heat shock protein 90
R Baruchello, D Simoni, G Grisolia… - Journal of medicinal …, 2011 - ACS Publications
A structural investigation on the isoxazole scaffold led to the discovery of 3, 4-
isoxazolediamide compounds endowed with potent Hsp90 inhibitory properties. We have …
isoxazolediamide compounds endowed with potent Hsp90 inhibitory properties. We have …
[HTML][HTML] 3D-QSAR study of combretastatin A-4 analogs based on molecular docking
Y Jin, P Qi, Z Wang, Q Shen, J Wang, W Zhang, H Song - Molecules, 2011 - mdpi.com
Combretastatin A-4 (CA-4), its analogues and their excellent antitumoral and antivascular
activities, have attracted considerable interest of medicinal chemists. In this article, a docking …
activities, have attracted considerable interest of medicinal chemists. In this article, a docking …
Synthesis, antiproliferative activities and in vitro biological evaluation of novel benzofuransulfonamide derivatives
In a cell-based screen of novel antiproliferative agents, the hit compound 1a, which bears a
benzofuransulfonamide scaffold, exhibited broad-spectrum antiproliferative activities against …
benzofuransulfonamide scaffold, exhibited broad-spectrum antiproliferative activities against …