delanzomib and Neoplasms

delanzomib has been researched along with Neoplasms* in 1 studies

Other Studies

1 other study(ies) available for delanzomib and Neoplasms

Article	Year
Azobenzene-containing photoswitchable proteasome inhibitors with selective activity and cellular toxicity. Bioorganic & medicinal chemistry, 2017, 10-01, Volume: 25, Issue:19 A series of azobenzene-containing peptidic boronate esters was prepared and the activity of the thermally adapted states (TAS), enriched in trans isomer, and the photostationary states (PSS), enriched in cis isomer, for each compound were evaluated against β5 and β1 proteasome subunits. Compounds with a sterically demanding phenyl-substituted azobenzene at P2 (4c), and a less sterically demanding unsubstituted azobenzene at the N-terminus (5a), showed the greatest difference in activity between the two states. In both cases, the more active trans-enriched TAS had activity comparable to bortezomib and delanzomib. Furthermore, cis-enriched 4c inhibited tumor growth in both breast and colorectal carcinoma cell lines. Significantly, the initial trans-enriched TAS of 4c was not cytotoxic against the non-malignant MCF-10A cells. Topics: Antineoplastic Agents; Azo Compounds; Cell Line, Tumor; Cell Proliferation; Humans; Isomerism; Neoplasms; Photochemical Processes; Proteasome Endopeptidase Complex; Proteasome Inhibitors	2017

Article

Year

Azobenzene-containing photoswitchable proteasome inhibitors with selective activity and cellular toxicity.

Bioorganic & medicinal chemistry, 2017, 10-01, Volume: 25, Issue:19

A series of azobenzene-containing peptidic boronate esters was prepared and the activity of the thermally adapted states (TAS), enriched in trans isomer, and the photostationary states (PSS), enriched in cis isomer, for each compound were evaluated against β5 and β1 proteasome subunits. Compounds with a sterically demanding phenyl-substituted azobenzene at P2 (4c), and a less sterically demanding unsubstituted azobenzene at the N-terminus (5a), showed the greatest difference in activity between the two states. In both cases, the more active trans-enriched TAS had activity comparable to bortezomib and delanzomib. Furthermore, cis-enriched 4c inhibited tumor growth in both breast and colorectal carcinoma cell lines. Significantly, the initial trans-enriched TAS of 4c was not cytotoxic against the non-malignant MCF-10A cells.

Topics: Antineoplastic Agents; Azo Compounds; Cell Line, Tumor; Cell Proliferation; Humans; Isomerism; Neoplasms; Photochemical Processes; Proteasome Endopeptidase Complex; Proteasome Inhibitors

2017