sk-7041 and Neoplasms

sk-7041 has been researched along with Neoplasms* in 2 studies

Reviews

1 review(s) available for sk-7041 and Neoplasms

Article	Year
Histone deacetylase inhibitors: from bench to clinic. Journal of medicinal chemistry, 2008, Mar-27, Volume: 51, Issue:6 Topics: Animals; Antineoplastic Agents; Cell Proliferation; Clinical Trials, Phase I as Topic; Clinical Trials, Phase II as Topic; Enzyme Inhibitors; Histone Deacetylase Inhibitors; Humans; Molecular Structure; Neoplasms	2008

Other Studies

1 other study(ies) available for sk-7041 and Neoplasms

Article	Year
Class I histone deacetylase-selective novel synthetic inhibitors potently inhibit human tumor proliferation. Clinical cancer research : an official journal of the American Association for Cancer Research, 2004, Aug-01, Volume: 10, Issue:15 We have developed previously a class of synthetic hybrid histone deacetylase (HDAC) inhibitors, which were built from hydroxamic acid of trichostatin A and pyridyl ring of MS-275. In this study we evaluated the antitumor effects of these novel hybrid synthetic HDAC inhibitors, SK-7041 and SK-7068, on human cancer cells. Both SK-7041 and SK-7068 effectively inhibited cellular HDAC activity at nanomolar concentrations and induced the time-dependent hyperacetylation of histones H3 and H4. These HDAC inhibitors preferentially inhibited the enzymatic activities of HDAC1 and HDAC2, as compared with the other HDAC isotypes, indicating that class I HDAC is the major target of SK-7041 and SK-7068. We found that these compounds exhibited potent antiproliferative activity against various human cancer cells in vitro. Growth inhibition effect of SK-7041 and SK-7068 was related with the induction of aberrant mitosis and apoptosis in human gastric cancer cells. Both compounds induced the accumulation of cells at mitosis after 6 h of treatment, which was demonstrated by accumulation of tetraploid cells, lack of G(2) cyclin/cyclin-dependent kinase inactivation, and higher mitotic index. After 12 h of treatment, apoptotic cells were increased through mitochondrial and caspase-mediated pathway. Finally, in vivo experiment showed that SK-7041 or SK-7068 was found to reduce the growth of implanted human tumors in nude mice. Therefore, based on isotype specificity and antitumor activity, SK-7041 and SK-7068 HDAC inhibitors are expected to be promising anticancer therapeutic agents and need additional clinical development. Topics: Amides; Animals; Antineoplastic Agents; Apoptosis; Biphenyl Compounds; Cell Line, Tumor; Cell Nucleus; Cell Proliferation; DNA; Dose-Response Relationship, Drug; Enzyme Inhibitors; Histone Deacetylase 1; Histone Deacetylase 2; Histone Deacetylase Inhibitors; Histones; Humans; Immunoblotting; Immunoprecipitation; Inhibitory Concentration 50; Mice; Mice, Nude; Mitosis; Models, Chemical; Neoplasm Transplantation; Neoplasms; Pyrrolidines; Repressor Proteins; Stomach Neoplasms; Time Factors	2004

Article

Year

Class I histone deacetylase-selective novel synthetic inhibitors potently inhibit human tumor proliferation.

Clinical cancer research : an official journal of the American Association for Cancer Research, 2004, Aug-01, Volume: 10, Issue:15

We have developed previously a class of synthetic hybrid histone deacetylase (HDAC) inhibitors, which were built from hydroxamic acid of trichostatin A and pyridyl ring of MS-275. In this study we evaluated the antitumor effects of these novel hybrid synthetic HDAC inhibitors, SK-7041 and SK-7068, on human cancer cells. Both SK-7041 and SK-7068 effectively inhibited cellular HDAC activity at nanomolar concentrations and induced the time-dependent hyperacetylation of histones H3 and H4. These HDAC inhibitors preferentially inhibited the enzymatic activities of HDAC1 and HDAC2, as compared with the other HDAC isotypes, indicating that class I HDAC is the major target of SK-7041 and SK-7068. We found that these compounds exhibited potent antiproliferative activity against various human cancer cells in vitro. Growth inhibition effect of SK-7041 and SK-7068 was related with the induction of aberrant mitosis and apoptosis in human gastric cancer cells. Both compounds induced the accumulation of cells at mitosis after 6 h of treatment, which was demonstrated by accumulation of tetraploid cells, lack of G(2) cyclin/cyclin-dependent kinase inactivation, and higher mitotic index. After 12 h of treatment, apoptotic cells were increased through mitochondrial and caspase-mediated pathway. Finally, in vivo experiment showed that SK-7041 or SK-7068 was found to reduce the growth of implanted human tumors in nude mice. Therefore, based on isotype specificity and antitumor activity, SK-7041 and SK-7068 HDAC inhibitors are expected to be promising anticancer therapeutic agents and need additional clinical development.

Topics: Amides; Animals; Antineoplastic Agents; Apoptosis; Biphenyl Compounds; Cell Line, Tumor; Cell Nucleus; Cell Proliferation; DNA; Dose-Response Relationship, Drug; Enzyme Inhibitors; Histone Deacetylase 1; Histone Deacetylase 2; Histone Deacetylase Inhibitors; Histones; Humans; Immunoblotting; Immunoprecipitation; Inhibitory Concentration 50; Mice; Mice, Nude; Mitosis; Models, Chemical; Neoplasm Transplantation; Neoplasms; Pyrrolidines; Repressor Proteins; Stomach Neoplasms; Time Factors

2004