ic9564 and Inflammation

ic9564 has been researched along with Inflammation* in 1 studies

Other Studies

1 other study(ies) available for ic9564 and Inflammation

Article	Year
New betulinic acid derivatives as potent proteasome inhibitors. Bioorganic & medicinal chemistry letters, 2011, Oct-01, Volume: 21, Issue:19 In this study, 22 new betulinic acid (BA) derivatives were synthesized and tested for their inhibition of the chymotrypsin-like activity of 20S proteasome. From the SAR study, we concluded that the C-3 and C-30 positions are the pharmacophores for increasing the proteasome inhibition effects, and larger lipophilic or aromatic side chains are favored at these positions. Among the BA derivatives tested, compounds 13, 20, and 21 showed the best proteasome inhibition activity with IC(50) values of 1.42, 1.56, and 1.80 μM, respectively, which are three to fourfold more potent than the proteasome inhibition controls LLM-F and lactacystin. Topics: Antineoplastic Agents; Betulinic Acid; Chymotrypsin; Cysteine Proteinase Inhibitors; Drug Design; Inflammation; Molecular Structure; Molecular Targeted Therapy; Neoplasms; Pentacyclic Triterpenes; Proteasome Inhibitors; Signal Transduction; Structure-Activity Relationship; Triterpenes	2011

Article

Year

New betulinic acid derivatives as potent proteasome inhibitors.

Bioorganic & medicinal chemistry letters, 2011, Oct-01, Volume: 21, Issue:19

In this study, 22 new betulinic acid (BA) derivatives were synthesized and tested for their inhibition of the chymotrypsin-like activity of 20S proteasome. From the SAR study, we concluded that the C-3 and C-30 positions are the pharmacophores for increasing the proteasome inhibition effects, and larger lipophilic or aromatic side chains are favored at these positions. Among the BA derivatives tested, compounds 13, 20, and 21 showed the best proteasome inhibition activity with IC(50) values of 1.42, 1.56, and 1.80 μM, respectively, which are three to fourfold more potent than the proteasome inhibition controls LLM-F and lactacystin.

Topics: Antineoplastic Agents; Betulinic Acid; Chymotrypsin; Cysteine Proteinase Inhibitors; Drug Design; Inflammation; Molecular Structure; Molecular Targeted Therapy; Neoplasms; Pentacyclic Triterpenes; Proteasome Inhibitors; Signal Transduction; Structure-Activity Relationship; Triterpenes

2011