Relevant articles and documents
All total 38 Articles be found
Design, synthesis, and cytotoxicity of novel 2,4,6-trisubstituted 1,3,5-triazines bearing aryl hydrazone moiety as potent antitumor agent
Wang, Limei,Zhao, Sijia,Bao, Guanglong,Zhang, Yu,Xi, Shuancheng,Zhou, Guolin,Zhai, Xin,Gong, Ping
, p. 621 - 630 (2016/10/18)
A novel series of 2,4,6-trisubstituted 1,3,5-triazine derivatives bearing aryl hydrazone moiety were designed and synthesized under the guidance of scaffold hopping and bioisosterism from the autophagy inhibitor VLX600. The target compounds were evaluated for cytotoxicity against HT-29 by MTT assay with VLX600 as positive control. Then, ten potent target compounds (5c-5f, 5i-5r, 5s, 5t) were further evaluated against two cancer cell lines H460 and A549 and one normal cell line WI-38. Most of them exhibited significant cytotoxicity against one or more cell lines. Particularly, a promising compound 5f was identified, which exhibited the most potent cytotoxicity against HT-29, H460 and A549 cancer cell lines with IC50 values of 0.047 μM, 0.071 μM and 0.071 μM, respectively, which was 10-to 62-folds more potent than VLX600 (IC50 = 0.47 μM, 4.1 μM, 4.4 μM). The preliminary structure-activity relationships (SARs) of the compounds were also discussed.
Targeting the hydrophobic region of Hsp90's ATP binding pocket with novel 1,3,5-triazines
Lee, Taeho,Seo, Young Ho
supporting information, p. 6427 - 6431 (2013/11/19)
Heat shock protein 90 (Hsp90) is a molecular chaperone that plays an important role in regulating the maturation and stabilization of many oncogenic proteins. In an attempt to discover a new class of Hsp90 inhibitors, a series of 1,3,5-triazine compounds were rationally designed, synthesized, and their biological activities were evaluated. Compound 3b was found to degrade Hsp90's client proteins of Her2, Met and Akt and to induce the expression level of Hsp70. The binding mode of 3b in the ATP-binding site of Hsp90 was predicted by the molecular docking.
Photochemical Crosslinkers for Polymer Coatings and Substrate Tie-Layer
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, (2008/06/13)
The invention describes novel crosslinking compounds that include photoactivatable moieties. Several families of compounds are disclosed that can include one or more hydrophilic moieties that help to solubilize the compounds in aqueous environments.