1053655-57-4Relevant articles and documents
Synthesis and biological evaluation of novel N-substituted benzamides as anti-migration agents for treatment of osteosarcoma
Chen, Xiaojing,Wang, Guangbao,Mohammed Alsayed, Ali Mohammed,Du, Zongxuan,Lu liu,Ma, Yue,Liu, Peng,Zhang, Qianwen,Chen, Xianxin,Chen, Wenbin,Ye, Faqing,Zheng, Xiaohui,Liu, Zhiguo
, (2021)
A novel series of novel N-substituted (indole or indazole) benzamides were synthesized, and their anti-tumor properties were evaluated. The majority of tested compounds possessed moderate cytotoxicity, but inspiringly, we verified that active compound 5d presents an astonishing advantage by inhibiting the adhesion, migration, and invasion of osteosarcoma (OS) cells in vitro. Mechanistically, we confirmed 5d inhibited the migration ability of OS cells via the expression of genes related to adhesion, migration, and invasion. This effects of 5d suggest that it can be used as a potential chemotherapeutic drug to some aggressive and/or metastatic cancers, as well as in combination with other clinical anti-cancer drugs. In turn, this could enhance the therapeutic effect or reduce the risk of cell migration.
RAS INHIBITORS AND METHODS OF USING THE SAME
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Paragraph 000150, (2021/08/06)
Provided herein are compounds identified as inhibitors of KRAS protein activity that can be used to treat various diseases and disorders, such as cancer.
Compound C18, preparation method thereof and application of the compound C18 in preparation of anti-lung cancer drugs
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, (2020/07/12)
The invention discloses a small molecular compound C18 and application thereof in preparation of anti-lung cancer drugs. The structural formula of the C18 is shown in the specification. Experimental results show that C18 can inhibit proliferation and clon
Structure-based design of a novel series of potent, selective inhibitors of the class i phosphatidylinositol 3-kinases
Smith, Adrian L.,D'Angelo, Noel D.,Bo, Yunxin Y.,Booker, Shon K.,Cee, Victor J.,Herberich, Brad,Hong, Fang-Tsao,Jackson, Claire L. M.,Lanman, Brian A.,Liu, Longbin,Nishimura, Nobuko,Pettus, Liping H.,Reed, Anthony B.,Tadesse, Seifu,Tamayo, Nuria A.,Wurz, Ryan P.,Yang, Kevin,Andrews, Kristin L.,Whittington, Douglas A.,McCarter, John D.,Miguel, Tisha San,Zalameda, Leeanne,Jiang, Jian,Subramanian, Raju,Mullady, Erin L.,Caenepeel, Sean,Freeman, Daniel J.,Wang, Ling,Zhang, Nancy,Wu, Tian,Hughes, Paul E.,Norman, Mark H.
, p. 5188 - 5219 (2012/08/28)
A highly selective series of inhibitors of the class I phosphatidylinositol 3-kinases (PI3Ks) has been designed and synthesized. Starting from the dual PI3K/mTOR inhibitor 5, a structure-based approach was used to improve potency and selectivity, resulting in the identification of 54 as a potent inhibitor of the class I PI3Ks with excellent selectivity over mTOR, related phosphatidylinositol kinases, and a broad panel of protein kinases. Compound 54 demonstrated a robust PD-PK relationship inhibiting the PI3K/Akt pathway in vivo in a mouse model, and it potently inhibited tumor growth in a U-87 MG xenograft model with an activated PI3K/Akt pathway.