118802-40-7Relevant academic research and scientific papers
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer
Yang, Zhuang,Wang, Taijin,Wang, Fang,Niu, Ting,Liu, Zhuowei,Chen, Xiaoxin,Long, Chaofeng,Tang, Minghai,Cao, Dong,Wang, Xiaoyan,Xiang, Wei,Yi, Yuyao,Ma, Liang,You, Jingsong,Chen, Lijuan
, p. 1455 - 1470 (2016/03/08)
Novel selective histone deacetylase 6 (HDAC6) inhibitors using the quinazoline as the cap were designed, synthesized, and evaluated for HDAC enzymatic assays. N-Hydroxy-4-(2-methoxy-5-(methyl(2-methylquinazolin-4-yl)amino)phenoxy)butanamide, 23bb, was the
Structure-activity relationship and in vitro and in vivo evaluation of the potent cytotoxic anti-microtubule agent N-(4-methoxyphenyl)-N,2,6-trimethyl-6,7- dihydro-5H-cyclopenta[d]pyrimidin-4-aminium chloride and its analogues as antitumor agents
Gangjee, Aleem,Zhao, Ying,Raghavan, Sudhir,Rohena, Cristina C.,Mooberry, Susan L.,Hamel, Ernest
, p. 6829 - 6844 (2013/10/01)
A series of 21 substituted cyclopenta[d]pyrimidines were synthesized as an extension of our discovery of the parent compound (±)-1·HCl as an anti-microtubule agent. The structure-activity relationship indicates that the N-methyl and a 4N-methoxy groups appear important for potent activity. In addition, the 6-substituent in the parent analogue is not necessary for activity. The most potent compound 30·HCl was a one to two digit nanomolar inhibitor of most tumor cell proliferations and was up to 7-fold more potent than the parent compound (±)-1·HCl. In addition, 30·HCl inhibited cancer cell proliferation regardless of Pgp or βIII-tubulin status, both of which are known to cause clinical resistance to several anti-tubulin agents. In vivo efficacy of 30·HCl was demonstrated against a triple negative breast cancer xenograft mouse model. Compound 30·HCl is water-soluble and easily synthesized and serves as a lead compound for further preclinical evaluation as an antitumor agent.
HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF
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Page/Page column 77, (2013/08/28)
Provided herein are thiophene compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.
