109250-45-5Relevant academic research and scientific papers
New 1,3-dioxolane and 1,3-dioxane derivatives as effective modulators to overcome multidrug resistance
Schmidt, Matthias,Ungvari, Johannes,Gloede, Julia,Dobner, Bodo,Langner, Andreas
, p. 2283 - 2297 (2007/10/03)
Multidrug resistance (MDR) to antitumor agents represents a major obstacle to a successful chemotherapy of cancer. Overexpression of P-glycoprotein (p-gp) seems to be the major factor responsible for MDR. A large number of chemically unrelated compounds are known to interact with p-gp resulting in a decreasing resistance. In our efforts related to structure-activity studies of new potential MDR reversal agents we synthesized a series of compounds that differ in the aromatic core structure, the linker, and the basic moiety. For our search of new aromatic core structures we synthesized novel 2,2-diphenyl-1,3-dioxolane, 2,2- diphenyl-1,3-dioxane, and 4,5-diphenyl-1,3-dioxolane derivatives. A range of lipophilic linker structures and protonable basic moieties were synthesized and investigated to optimize the structure of the potential MDR-modulators. The compounds were tested in vitro using human Caco-2 cells. Both the cytotoxicity of the synthons and their ability to resensitize the cells were determined with a MTT assay. The results show that at low concentration various substances reverse tumor cell MDR. Some of the new structures show better effects than established modulators like trifluoperazine.
SIP3 RECEPTOR ANTAGONIST
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Page/Page column 20, (2010/02/14)
PROBLEM TO BE SOLVED: To obtain a compound having selective SIP3 receptor antagonism and a medicine containing the same. SOLUTION: The medicine comprises an aminopropionic acid derivative represented by general formula (1) (R1 is a hydrogen atom or a lower alkyl group; R2 is formula A; A is CO or CH2; E is an oxygen atom or an NR4; R3 is a lower alkyl group or formula B; G is CH, a nitrogen atom or a phosphorus atom; J is an oxygen atom or a sulfur atom; R4 is a hydrogen atom or a lower alkyl group; R5, R6 and R7 are each the same or different and a hydrogen atom, a lower alkyl group, a lower alkoxy group, a halogen atom, a nitro group or a haloalkyl group; m is an integer of 1-8; n is an integer of 1-5) or its pharmaceutically permissible salt as an active ingredient.
Reduction of activated thiopyridyl compounds by zinc metal
Boivin, Jean,Lallemand, Jean-Yves,Schmitt, Andreas,Zard, Samir Z.
, p. 7243 - 7246 (2007/10/02)
Starting from thiopyridyl compounds bearing a radical stabilizing group in α-position to the thiopyridyl moiety, the thiopyridyl group can be easily removed upon reduction by zinc metal in acetic acid.
