24941-58-0Relevant articles and documents
INHIBITORS OF TYROSINE KINASE
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Paragraph 00371, (2021/01/29)
The present disclosure provides compounds and compositions thereof which are useful as inhibitors of tyrosine kinase and which exhibit desirable characteristics for the same. Further disclosed herein are methods of treating cancer using these tyrosine kin
Synthesis of the oxa-bridged octalin system of two anti-anaerobe antibiotics, luminamicin and lustromycin
Sunazuka, Toshiaki,Handa, Masaki,Hirose, Tomoyasu,Matsumaru, Takanori,Togashi, Yuko,Nakamura, Kaoru,Iwai, Yuzuru,Omura, Satoshi
, p. 5297 - 5300 (2008/02/09)
An efficient, stereocontrolled entry to the 11-oxatricyclo[5.3.1.1,703,8]undecane nucleus of luminamicin and lustromycin was afforded via intramolecular hetero-Michael addition of enone 7 followed by intramolecular aldol condensation of aldehyde 5 by way of the epimerization at the stereocenter attached by the aldehyde group.
Conformationally restricted butyrophenones with mixed dopaminergic (D2) and serotoninergic (5-HT(2A)) affinities. Synthesis of 5-aminoethyl-and 6- aminomethyl-4-oxotetrahydroindoles as potential atypical antipsychotics
Masaguer, Christian F.,Casariego, Isabel,Ravina, Enrique
, p. 621 - 632 (2007/10/03)
We describe the synthesis of 5-aminoethyl- and 6-aminomethyl-4- oxotetrahydroindoles as butyrophenone derivatives in the indole series, as potential atypical antipsychotics. The affinities of these compounds for serotonin (5-HT(2A)) and dopamine (D2) receptors were evaluated in vitro. The ratios of pK(i)'s for 5-HT(2A)/D2 receptors may be useful for rapid screening of new compounds and assessing potential induction of extrapyramidal symptoms; ratio values ≥1.12 (Meltzer's ratio) are predictive of an atypical antipsychotic profile. Compounds 26e (QF 0408B) and 26f (QF 0409B) showed high affinity for both D2 and 5-HT(2A) receptors, and their Meltzer's ratios were 1.32 and 1.17 respectively, while haloperidol showed a ratio of 0.93.