796047-10-4Relevant academic research and scientific papers
COMPOSITIONS FOR THE TREATMENT OF HYPERTENSION AND/OR FIBROSIS
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, (2015/04/15)
The present invention relates to novel compounds and their use in the prophylactic and/or therapeutic treatment of hypertension and/or fibrosis.
Thiazolidinedione derivatives as PTP1B inhibitors with antihyperglycemic and antiobesity effects
Bhattarai, Bharat Raj,Kafle, Bhooshan,Hwang, Ji-Sun,Khadka, Deegendra,Lee, Sun-Myung,Kang, Jae-Seung,Ham, Seung Wook,Han, Inn-Oc,Park, Hwangseo,Cho, Hyeongjin
supporting information; experimental part, p. 6161 - 6165 (2010/06/16)
Benzylidene-2,4-thiazolidinedione derivatives with substitutions on the phenyl ring at the ortho or para positions of the thiazolidinedione (TZD) group were synthesized as PTP1B inhibitors with IC50 values in a low micromolar range. Compound 3e, the lowest, bore an IC50 of 5.0 μM. In vivo efficacy of 3e as an antiobesity and hypoglycemic agent was evaluated in a mouse model system. Significant improvement of glucose tolerance was observed. This compound also significantly suppressed weight gain and significantly improved blood parameters such as TG, total cholesterol and NEFA. Compound 3e was also found to activate peroxisome proliferator-activated receptors (PPARs) indicating multiple mechanisms of action.
Synthesis and biological evaluation of rhodanine derivatives as PRL-3 inhibitors
Ahn, Jin Hee,Kim, Seung Jun,Park, Woul Seong,Cho, Sung Yun,Ha, Jae Du,Kim, Sung Soo,Kang, Seung Kyu,Jeong, Dae Gwin,Jung, Suk-Kyeong,Lee, Sang-Hyeup,Kim, Hwan Mook,Park, Song Kyu,Lee, Ki Ho,Lee, Chang Woo,Ryu, Seong Eon,Choi, Joong-Kwon
, p. 2996 - 2999 (2008/09/20)
A series of rhodanine derivatives was synthesized and evaluated for their ability to inhibit PRL-3. Benzylidene rhodanine derivative showed good biological activity, while compound 5e was the most active in this series exhibiting an IC50 value of 0.9 μM in vitro and showed a reduced invasion in cell-based assay.
Synthesis and biological evaluation of thiazolidine-2,4-dione and 2,4-thione derivatives as inhibitors of translation initiation
Chen, Han,Fan, Yun-Hua,Natarajan, Amarnath,Guo, Yuhong,Iyasere, Julia,Harbinski, Fred,Luus, Lia,Christ, William,Aktas, Huseyin,Halperin, Jose A.
, p. 5401 - 5405 (2007/10/03)
A series of 2′-benzyloxy-5′-substituted-5-benzylidene- thiazolidine-2,4-thione and -dione derivatives was synthesized and evaluated as inhibitors of translation initiation. In an effort to generate novel translation initiation inhibitors for cancer therapy, a series of 2′-benzyloxy- 5′-substituted-5-benzylidene-thiazolidine-2,4-thione and dione derivatives was synthesized and evaluated for activity in translation initiation specific assays. Several candidates of the 5-benzylidene-thiazolidine-2,4-diones (3c, 3d, and 3f) and -thiones (2b, 2e, and 2j), inhibit cell growth with low μM GI50 mediated by inhibition of translation initiation, which involves partial depletion of intracellular Ca2+ stores and strong phosphorylation of eIF2Iα.
