bevirimat and Neoplasms

bevirimat has been researched along with Neoplasms* in 2 studies

Other Studies

2 other study(ies) available for bevirimat and Neoplasms

Article	Year
A-ring modified betulinic acid derivatives as potent cancer preventive agents. Bioorganic & medicinal chemistry letters, 2014, Feb-01, Volume: 24, Issue:3 Ten new 3,4-seco betulinic acid (BA) derivatives were designed and synthesized. Among them, compounds 7-15 exhibited enhanced chemopreventive ability in an in vitro short-term 12-O-tetradecanoylphorbol-13-acetate (TPA) induced Epstein-Barr virus early antigen (EBV-EA) activation assay in Raji cells. Specifically, analogs with a free C-28 carboxylic acid, including 7, 8, 11, and 13, inhibited EBV-EA activation significantly. The most potent compound 8 displayed 100% inhibition at 1×10(3) mol ratio/TPA and 73.4%, 35.9%, and 8.4% inhibition at 5×10(2), 1×10(2), and 1×10 mol ratio/TPA, respectively, comparable with curcumin at high concentration and better than curcumin at low concentration. The potent chemopreventive activity of novel seco A-ring BAs (8 and 11) was further confirmed in an in vivo mouse skin carcinogenesis assay. Topics: Animals; Anticarcinogenic Agents; Betulinic Acid; Cell Line; Herpesvirus 4, Human; Humans; Mice; Neoplasms; Pentacyclic Triterpenes; Triterpenes	2014
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

A-ring modified betulinic acid derivatives as potent cancer preventive agents.

Bioorganic & medicinal chemistry letters, 2014, Feb-01, Volume: 24, Issue:3

Ten new 3,4-seco betulinic acid (BA) derivatives were designed and synthesized. Among them, compounds 7-15 exhibited enhanced chemopreventive ability in an in vitro short-term 12-O-tetradecanoylphorbol-13-acetate (TPA) induced Epstein-Barr virus early antigen (EBV-EA) activation assay in Raji cells. Specifically, analogs with a free C-28 carboxylic acid, including 7, 8, 11, and 13, inhibited EBV-EA activation significantly. The most potent compound 8 displayed 100% inhibition at 1×10(3) mol ratio/TPA and 73.4%, 35.9%, and 8.4% inhibition at 5×10(2), 1×10(2), and 1×10 mol ratio/TPA, respectively, comparable with curcumin at high concentration and better than curcumin at low concentration. The potent chemopreventive activity of novel seco A-ring BAs (8 and 11) was further confirmed in an in vivo mouse skin carcinogenesis assay.

Topics: Animals; Anticarcinogenic Agents; Betulinic Acid; Cell Line; Herpesvirus 4, Human; Humans; Mice; Neoplasms; Pentacyclic Triterpenes; Triterpenes

2014

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