cortistatin-a and isoquinoline

cortistatin-a has been researched along with isoquinoline* in 2 studies

Other Studies

2 other study(ies) available for cortistatin-a and isoquinoline

Article	Year
Total synthesis of cortistatins A and J. The Journal of organic chemistry, 2011, Apr-15, Volume: 76, Issue:8 This paper describes the details of our synthetic studies on the marine steroidal alkaloids cortistatins A and J. The key features of our strategy include (i) an efficient Knoevenagel/electrocyclic strategy to couple the diketone and the CD-ring fragment, (ii) a chemoselective radical cyclization to construct the oxabicyclo[3.2.1]octene B-ring system, (iii) a highly stereocontrolled installation of the isoquinoline unit, and (iv) a late-stage functionalization of the A-ring. Topics: Alkaloids; Angiogenesis Inhibitors; Animals; Aquatic Organisms; Cyclization; Heterocyclic Compounds, 4 or More Rings; Isoquinolines; Ketones; Neovascularization, Pathologic; Neovascularization, Physiologic; Neuropeptides; Polycyclic Compounds; Porifera; Stereoisomerism; Steroids	2011
Total synthesis and biological evaluation of cortistatins A and J and analogues thereof. Journal of the American Chemical Society, 2009, Aug-05, Volume: 131, Issue:30 Total syntheses of the highly selective antiproliferative natural products cortistatins A (1) and J (5) in their naturally occurring enantiomeric forms are described. The modular and convergent strategy employed relies on an intramolecular oxa-Michael addition/aldol/dehydration cascade reaction to cast the ABCD ring framework of the molecule and both Sonogashira and Suzuki-Miyaura coupling reactions to assemble the necessary building blocks into the required heptacyclic skeleton. A divergent approach from a late-stage epoxy ketone leads to both target molecules in a stereoselective manner. The developed synthetic technologies were applied to the construction of several analogues of the cortistatins which were biologically evaluated and compared to the natural products with regards to their antiproliferative activities against a variety of cancer cells. Analogues 8 and 81, lacking both the dimethylamino and hydroxyl groups of cortistatin A, were found to exhibit comparable biological activity as the parent compound, leading to the conclusion that such functionalities are not essential for biological activity. Topics: Biological Products; Cell Line, Tumor; Cell Proliferation; Heterocyclic Compounds, 4 or More Rings; Humans; Inhibitory Concentration 50; Isoquinolines; Polycyclic Compounds	2009

Article

Year

Total synthesis of cortistatins A and J.

The Journal of organic chemistry, 2011, Apr-15, Volume: 76, Issue:8

This paper describes the details of our synthetic studies on the marine steroidal alkaloids cortistatins A and J. The key features of our strategy include (i) an efficient Knoevenagel/electrocyclic strategy to couple the diketone and the CD-ring fragment, (ii) a chemoselective radical cyclization to construct the oxabicyclo[3.2.1]octene B-ring system, (iii) a highly stereocontrolled installation of the isoquinoline unit, and (iv) a late-stage functionalization of the A-ring.

Topics: Alkaloids; Angiogenesis Inhibitors; Animals; Aquatic Organisms; Cyclization; Heterocyclic Compounds, 4 or More Rings; Isoquinolines; Ketones; Neovascularization, Pathologic; Neovascularization, Physiologic; Neuropeptides; Polycyclic Compounds; Porifera; Stereoisomerism; Steroids

2011

Total synthesis and biological evaluation of cortistatins A and J and analogues thereof.

Journal of the American Chemical Society, 2009, Aug-05, Volume: 131, Issue:30

Total syntheses of the highly selective antiproliferative natural products cortistatins A (1) and J (5) in their naturally occurring enantiomeric forms are described. The modular and convergent strategy employed relies on an intramolecular oxa-Michael addition/aldol/dehydration cascade reaction to cast the ABCD ring framework of the molecule and both Sonogashira and Suzuki-Miyaura coupling reactions to assemble the necessary building blocks into the required heptacyclic skeleton. A divergent approach from a late-stage epoxy ketone leads to both target molecules in a stereoselective manner. The developed synthetic technologies were applied to the construction of several analogues of the cortistatins which were biologically evaluated and compared to the natural products with regards to their antiproliferative activities against a variety of cancer cells. Analogues 8 and 81, lacking both the dimethylamino and hydroxyl groups of cortistatin A, were found to exhibit comparable biological activity as the parent compound, leading to the conclusion that such functionalities are not essential for biological activity.

Topics: Biological Products; Cell Line, Tumor; Cell Proliferation; Heterocyclic Compounds, 4 or More Rings; Humans; Inhibitory Concentration 50; Isoquinolines; Polycyclic Compounds

2009