94378-10-6Relevant academic research and scientific papers
Fascaplysin derivative as well as preparation method and application
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Paragraph 0021; 0036, (2018/04/21)
The invention discloses a fascaplysin derivative as well as a preparation method and application thereof to a drug. A general formula of the fascaplysin derivative disclosed by the invention is shownas a formula (I) and the formula (I) is shown in the description. The compound disclosed by the invention can be applied to preparation of drugs for preventing or treating diseases related to a cyclin-dependent kinase CDK4 inhibitor and anti-tumor drugs. The fascaplysin derivative keeps a pharmacodynamics effect of the CDK4 inhibitor; the compound has a high yield, is relatively stable in the air,has relatively good water solubility and is simple to operate; and the compound has the advantages of easiness for obtaining raw materials, low price, short preparation route, simple preparation method and low production cost.
Synthesis and evaluation of β-carbolinium cations as new antimalarial agents based on π-delocalized lipophilic cation (DLC) hypothesis
Takasu, Kiyosei,Shimogama, Tsubasa,Saiin, Chalerm,Kim, Hye-Sook,Wataya, Yusuke,Brun, Reto,Ihara, Masataka
, p. 653 - 661 (2007/10/03)
Several β-carbolines including naturally occurring substances and their corresponding cationic derivatives were synthesized and evaluated for antimalarial (antiplasmodial) activity in vitro and in vivo. A tetracyclic carbolinium salt was elucidated for antileishmanial and antitrypanosomal activities in vitro as well as antiplasmodial activity. Quarternary carbolinium cations showed much higher potencies in vitro than electronically neutral β-carbolines and a good correlation was observed between π-delocalized lipophilic cationic (DLC) structure and antimalarial efficacy. β-Carbolinium compounds exhibit medium suppressive activity in vivo against rodent malaria.
