Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: UMLS:C0017636 (
glioblastoma
)
18,345
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
Piplartine (
1
) is an alkamide extracted from plants of the genus
Piper
which shows several pharmacological properties, including antitumor activity. To improve this activity, a series of analogues based on
1
have been synthesized by esterification and amidation using the 3,4,5-trimethoxycinnamic acid-like starting material. During the study, the moieties 3-(3,4,5-trimethoxyphenyl)acrylate and
3-(3,4,5-trimethoxyphenyl)acrylamide
were maintained on esters and amides respectively. Meanwhile, functional changes were exploited, and it was revealed that the presence of two aromatic rings in the side-chain was important to improve the cytotoxic activity against the U87MG cell line, such as the compound (
E
)-benzhydryl 3-(3,4,5-trimethoxyphenyl)acrylate (
10
), an ester that exhibited strong cytotoxicity and a similar level of potency to that of paclitaxel, a positive control. Compound
10
had a marked concentration-dependent inhibitory effect on the viability of the U87MG cell line with apoptotic and oxidative processes, showing good potential for altering main molecular pathways to prevent tumor development. Moreover, it has strong bioavailability with non-genotoxic and non-cytotoxic properties on human blood cells. In conclusion, the findings of the present study demonstrated that compound
10
is a promising agent that may find applications combatting diseases associated with oxidative stress and as a prototype for the development of novel drugs used in the treatment of
glioblastoma
.
...
PMID:Piplartine Analogues and Cytotoxic Evaluation against Glioblastoma. 2989 Jun 17
