Novel CDKs inhibitors for the treatment of solid tumour by simultaneously regulating the cell cycle and transcription control was written by Wang, Xin;Deng, Kaiyuan;Wang, Cheng;Li, Yao;Wang, Tianqi;Huang, Zhi;Ma, Yakun;Sun, Peiqing;Shi, Yi;Yang, Shengyong;Fan, Yan;Xiang, Rong. And the article was included in Journal of Enzyme Inhibition and Medicinal Chemistry in 2020.Related Products of 954-81-4 This article mentions the following:
A novel series of cyclin-dependent kinases (CDKs) inhibitors, which play critical roles in the cell cycle control and regulation of cell transcription, were synthesized. A systematic study of enzymic and cellular assays led to the identification of compound with a nanomolar potency against CDK4 and CDK9 and potent antiproliferative activities against a panel of tumor cell lines. could induce cell cycle arrest and cell apoptosis in cancer cell lines. dose-dependently inhibits signalling pathways downstream of CDKs in cancer cells. In vivo antitumor activity assays, oral administration of led to significant tumor regression in mouse model without obvious toxicity. Superior anti-cancer efficacy in vitro and in vivo of demonstrated combined depletion of cell cycle and transcriptional CDK all contributed to antitumor activity. Taken together, concomitant inhibition of cell cycle and transcriptional CDK activities provided valuable guide for further structural optimization. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Related Products of 954-81-4).
N-(5-Bromopentyl)phthalimide (cas: 954-81-4) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. In the pharmaceutical industry organo bromine derivatives are used as sedatives, vasodilators, antiseptic agents, and anticancer agents.Related Products of 954-81-4
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary