71083-60-8Relevant academic research and scientific papers
Discovery of VU6027459: A First-in-Class Selective and CNS Penetrant mGlu7Positive Allosteric Modulator Tool Compound
Reed, Carson W.,Kalbfleisch, Jacob J.,Wong, Madison J.,Washecheck, Jordan P.,Hunter, Ashton,Rodriguez, Alice L.,Blobaum, Anna L.,Conn, P. Jeffrey,Niswender, Colleen M.,Lindsley, Craig W.
, p. 1773 - 1779 (2020/10/19)
Herein, we report the discovery of the first selective and CNS penetrant mGlu7 PAM (VU6027459) derived from a "molecular switch"within a selective mGlu7 NAM chemotype. VU6027459 displayed CNS penetration in both mice (Kp = 2.74) and rats (Kp= 4.78), it was orally bioavailable in rats (%F = 69.5), and undesired activity at DAT was ablated.
Synthesis and cytotoxicity studies of quinoline-3-carbonitrile derivatives
Zhang, Shu Lan,Zhai, Xin,Zhang, Shi Jiao,Yu, Hong Hao,Gong, Ping
scheme or table, p. 939 - 942 (2011/11/13)
A series of quinoline-3-carbonitrile derivatives were designed and synthesized. Their cytotoxicity in vitro against four cancer cell lines (A549, HT-29, MDA-MB-231 and SMMC-7721) were evaluated by standard MTT assay. The pharmacological results showed that most of the prepared compounds displayed excellent selective cytotoxicity toward SMMC-7721 cell line. Among them, compounds 7c, 7e, 11b, 11f and 11g were more active than Gefitinb against SMMC-7721 cell line.
