- Pyridine methylamino dithio formic acid heteroaryl naphthenic base ester compound and preparation method and application thereof
-
The invention relates to a compound as shown in a general formula (I) or pharmaceutically acceptable salts or solvates thereof, and relates to a preparation method of the compound and application thereof in preparing anti-tumor drugs. Please see the general formula (I) in the description.
- -
-
Paragraph 0167; 0168; 0169; 0183; 0184; 0185
(2017/01/02)
-
- Structure-activity relationship studies and biological characterization of human NAD+-dependent 15-hydroxyprostaglandin dehydrogenase inhibitors
-
The structure-activity relationship (SAR) study of two chemotypes identified as inhibitors of the human NAD+-dependent 15-hydroxyprostaglandin dehydrogenase (HPGD, 15-PGDH) was conducted. Top compounds from both series displayed potent inhibition (IC50 2 production in A549 lung cancer and LNCaP prostate cancer cells.
- Duveau, Damien Y.,Yasgar, Adam,Wang, Yuhong,Hu, Xin,Kouznetsova, Jennifer,Brimacombe, Kyle R.,Jadhav, Ajit,Simeonov, Anton,Thomas, Craig J.,Maloney, David J.
-
supporting information
p. 630 - 635
(2014/01/23)
-
- Narrow SAR in odorant sensing Orco receptor agonists
-
The systematic exploration of a series of triazole-based agonists of the cation channel insect odorant receptor is reported. The structure-activity relationships of independent sections of the molecules are examined. Very small changes to the compound structure were found to exert a large impact on compound activity. Optimal substitutions were combined using a 'mix-and-match' strategy to produce best-in-class compounds that are capable of potently agonizing odorant receptor activity and may form the basis for the identification of a new mode of insect behavior modification.
- Romaine, Ian M.,Taylor, Robert W.,Saidu, Samsudeen P.,Kim, Kwangho,Sulikowski, Gary A.,Zwiebel, Laurence J.,Waterson, Alex G.
-
p. 2613 - 2616
(2014/06/09)
-
- Synthesis of 2-Alkylputrescines from 3-Alkylpyrroles
-
Acylation of 2-(trichloroacetyl)pyrrole gave the 4-acyl derivatives (from 4-formyl to 4-hexanoyl) in good yields.Alkaline treatment gave corresponding 4-acyl-2-pyrrolecarboxylic acids, were decarboxylated to the 3-acylpyrroles by prior conversion to the 3-acyl-2,4,5-triiodopyrroles followed by hydrogenolysis.The 3-acylpyrroles were reduced by treatment with hydrazine in alkaline medium to the 3-alkylpyrroles.The latter were ring-opened by treatment with hydroxylamine in the presence of bicarbonate to give the dioximes of the corresponding 2-alkylsuccinaldehydes, which were then reduced to the 2-alkylpurescines (1,4-diaminobutanes).Ring-opening of 2,3-dimethylpyrrole followed by reduction of the dioxime gave 1,2-dimethylputrescine; the same sequence gave 1,3-dimethylputrescine from 2,4-dimethylpyrrole, while 3,4-dimethylpyrrole did not ring-open and gave the dioxime of 3,4-dimethylmaleimide.
- Garrido, Daniel O. A.,Buldain, Graciela,Ojea, Maria I.,Frydman, Benjamin
-
p. 403 - 407
(2007/10/02)
-