20075-26-7Relevant articles and documents
Assembly of the active center of organophosphorus hydrolase in metal-organic frameworks: Via rational combination of functional ligands
Xia, Mengfan,Zhuo, Caixia,Ma, Xuejuan,Zhang, Xiaohong,Sun, Huaming,Zhai, Quanguo,Zhang, Yaodong
, p. 11302 - 11305 (2017)
Different from popular mimics of bimetallic nuclear centers bridged by a hydroxide, a total coordination sphere of the active center of organophosphorus hydrolase was assembled in metal-organic frameworks by rational design and combination of ligands, which resulted in efficient destruction of nerve agent stimulants without a base as a co-catalyst.
Synthetic studies on dragmacidin D: Synthesis and assembly of three fragments towards an advanced intermediate
Oikawa, Masato,Ikoma, Minoru,Sasaki, Makoto
experimental part, p. 4654 - 4666 (2011/10/03)
We report herein the approach to the key advanced intermediate in the synthesis of the bioactive marine natural product dragmacidin D. By employing a modular synthesis strategy of three fragments (5, 7, and 8), the advanced intermediate 3 has been successfully synthesized in 2.5% yield over 15 steps by starting from nitrotoluene 20. The synthesis also involves sequential cross-coupling reactions, namely Sonogashira and Suzuki-Miyaura reactions, so that various analogues can be efficiently synthesized, which will allow the study of structure-activity relationships of dragmacidin D.
BIOACTIVE COMPOUNDS FOR TREATMENT OF CANCER AND NEURODEGENERATIVE DISEASES
-
Page/Page column 142-143, (2009/12/23)
The invention provides bioactive compounds for the treatment of various malconditions such as cancer and neurodegenerative diseases including Alzheimer's disease. The chemical compounds as disclosed herein are found to show bioactivity in bioassays related to these conditions. Pharmaceutical compositions, combinations and methods of synthesis are provided, as are methods of using the compound, compositions and combinations in the treatment of the diseases.
N-HETEROCYCLYL-SUBSTITUTED AMINO-THIAZOLE DERIVATIVES AS PROTEIN KINASE INHIBITORS
-
Page 121, (2010/02/08)
Aminothiazole compounds with N-containing cycloalkyl at the 2-amino position which are represented by the Formula (I), or a pharmaceutically acceptable prodrug of said compound, or pharmaceutically acceptable salt of said compound, modulate and/or inhibit the cell proliferation and activity of protein kinases.
Arylsulfonamidobenzylic compounds
-
Page 20, (2010/02/05)
Arylsulfonamidobenzyl alcohols, amines and sulfonamides are provided which are useful in treating lipid disorders, metabolic diseases and cell-proliferative diseases.
1,2,3-Benzothiadiazole derivatives
-
, (2008/06/13)
Novel 1,2,3-benzothiadiazole derivatives of the formula STR1 in which Het has the meanings set forth in the specification, and addition products thereof with an acid or metal salt are very effective for the control of undesired microorganisms. Novel intermediates of the formulae STR2 in which Het1 and R5 have the meanings given in the specification.
Chloropyridylcarbonyl derivatives
-
, (2008/06/13)
Novel chloropyridylcarbonyl derivatives of the formula STR1 in which Het is STR2 n is 1 or 2, R1 is hydrogen, optionally substituted C1-6 alkyl, optionally substituted C2-6 alkenyl, optionally substituted C3-6 alkynyl, optionally substituted phenyl or optionally substituted pyrimidinyl, and R2 and R3, independently of each other, are hydrogen or C1-4 alkyl, and acid addition salts and metal salt complexes thereof, are outstandingly active as microbicides.
Camptothecin and minor-groove binder hybrid molecules: Synthesis, inhibition of topoisomerase I, and anticancer cytotoxicity in vitro
Zhao,Al-Said,Sternbach,Lown
, p. 216 - 225 (2007/10/03)
The synthesis, characterization, inhibitory activity against topoisomerase I, and biological evaluation of a series of 14 camptothecin derivatives of polypyrrolecarboxamide (lexitropsin) conjugates of two structural classes: (A) camptothecin-NHCO-lexitropsin 44-51 and (B) camptothecin-CONH-lexitropsin 38-43 are described. All 16 compounds tested, 14 conjugates plus two functionalized camptothecin controls, inhibit topoisomerase I in the concentration range 1.12-16.6 μM that divide into three distinct categories based on activity. The most active enzyme inhibitors belong to structure class A with either cationic dimethylaminium or neutral amide end groups. Generally class B conjugates are less effective in inhibiting topoisomerase I. Cytotoxic potencies of the drugs was tested against four representative human tumor cell lines: SKOV3, SKLVB, HT29, and KB. All 16 drugs gave measurable IC50 values against the KB cell line and fell into two categories with IC50 values of 0.049-0.66 μM (largely structure class B) and 1.0-48 μM (largely class A). Thus the class B conjugates, while less potent against the enzyme, contain two of the most potent drugs, 38 and 39, against KB cell lines. In contrast, in the case of the cell lines SKOV3 and HT29 there was a general correlation between the better topoisomerase inhibitors and their cell cytotoxicities.
Cyclopropylpyrroloindole-oligopeptide anticancer agents
-
, (2008/06/13)
The invention is directed to novel cyclopropylpyrroloindole-oligopeptide compounds which are useful as anticancer agents. The novel cyclopropylpyrroloindole-oligopeptide compounds have the following general structure: STR1 wherein, Het1 and Het2 are individually selected from the group consisting of pyrrole, imidazole, triazole, thiophene, furan, thiazole, oxazole and pyrazole, R is selected from the group consisting of a valence bond; a C1 -C6 alkyl; a C2 -C6 alkenyl; a C2 -C6 alkynyl; and an ortho, meta or para linked aromatic group, A is selected from the group consisting of a C1 -C6 alkyl group; an amidine or derivative thereof; a guanidine; a secondary, tertiary or quaternary ammonium salt; and a sulfonium salt, n is 0 to 3, and m is 0 to 3.