- Directed β C-H Amination of Alcohols via Radical Relay Chaperones
-
A radical-mediated strategy for β C-H amination of alcohols has been developed. This approach employs a radical relay chaperone, which serves as a traceless director that facilitates selective C-H functionalization via 1,5-hydrogen atom transfer (HAT) and enables net incorporation of ammonia at the β carbon of alcohols. The chaperones presented herein enable direct access to imidate radicals, allowing their first use for H atom abstraction. A streamlined protocol enables rapid conversion of alcohols to their β-amino analogs (via in situ conversion of alcohols to imidates, directed C-H amination, and hydrolysis to NH2). Mechanistic experiments indicate HAT is rate-limiting, whereas intramolecular amination is product- and stereo-determining.
- Wappes, Ethan A.,Nakafuku, Kohki M.,Nagib, David A.
-
p. 10204 - 10207
(2017/08/10)
-
- Thiazolinone unsubstituted quinolines
-
Thiazolinone quinoline derivatives having no substitution on the quinoline ring active as CDK1 inhibitors which are useful as anti-proliferation agents such as for treating solid tumors.
- -
-
Page/Page column 14
(2010/02/15)
-
- PYRAZOLE DERIVATIVES AS INHIBITORS OF RECEPTOR TYROSYNE KINASES
-
Compounds of formula (I): and their use in the inhibition of Trk activity are described.
- -
-
Page/Page column 114
(2008/06/13)
-
- THIADIAZOLEDIOXIDES AND THIADIAZOLEOXIDES AS CXC- AND CC-CHEMOKINE RECEPTOR LIGANDS
-
Disclosed are novel compounds of the formula (IA) and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, acute pain, acute and chronic inflammatory pain, and neuropathic pain using a compound of formula (IA).
- -
-
-
- Novel diarylsulfonylurea derivatives as potent antimitotic agents
-
Novel diarylsulfonylurea derivatives have been synthesized and identified as potent inhibitors of tubulin polymerization and cancer cell proliferation. Furthermore, these compounds were also efficacious against multidrug-resistant cancer cells. A novel series of diarylsulfonylurea derivatives were synthesized and evaluated for interaction with tubulin and for cytotoxicity against human cancer cell lines. These derivatives demonstrated good inhibitory activity against tubulin polymerization, which was well correlated with promising antiproliferative activity as well as G2/M phase cell cycle arrest. Furthermore, several compounds were also efficacious against multidrug-resistant cancer cells, which are resistant to many other known microtubule inhibitors.
- Kim, Semi,Park, Ji Hyun,Koo, Sun-Young,Kim, Jung In,Kim, Min-Hyeung,Kim, Ji Eun,Jo, Kiwon,Geun Choi, Hwan,Lee, Sung Bae,Jung, Sang-Hun
-
p. 6075 - 6078
(2007/10/03)
-
- 3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands
-
There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.
- -
-
-