504404-56-2Relevant academic research and scientific papers
Design, synthesis and biological evaluation of pyrimidine derivatives as novel CDK2 inhibitors that induce apoptosis and cell cycle arrest in breast cancer cells
Wang, Yiting,Chen, Yanmei,Cheng, Xiaoling,Zhang, Ke,Wang, Hangyu,Liu, Bo,Wang, Jinhui
, p. 3491 - 3501 (2018)
Cyclin-dependent kinase 2 (CDK2) plays a key role in eukaryotic cell cycle progression which could facilitate the transition from G1 to S phase. The dysregulation of CDK2 is closely related to many cancers. CDK2 is utilized as one of the most studied kina
Discovery of a novel small-molecule inhibitor of Fam20C that induces apoptosis and inhibits migration in triple negative breast cancer
Chen, Lixia,Chen, Yanmei,Fu, Leilei,Liu, Bo,Liu, Yi,Sun, Dejuan,Wang, Leiming,Yuan, Zhaoxin,Zhang, Kai,Zhang, Lan,Zhao, Rongyan
, (2020/12/21)
The family with sequence similarity 20, member C (Fam20C), a Golgi casein kinase, has been recently regarded as a potential therapeutic target for the treatment of triple negative breast cancer (TNBC). Lacking enzyme activity center has been becoming an obstacle to the development of small-molecule inhibitors of Fam20C. Herein, we combined in silico high-throughput screening with chemical synthesis methods to obtain a new small-molecule Fam20C inhibitor 3r, which exhibited desired anti-proliferative activities against MDA-MB-231 cells and also inhibited migration. Subsequently, the enzymatic assay, molecular docking, and molecular dynamics (MD) simulations were carried out for validating that 3r could bind to Fam20C. In addition, 3r was found to induce apoptosis via the mitochondrial pathway in MDA-MB-231 cells as well as to inhibit cell migration. Moreover, we demonstrated that 3r inhibited tumor growth in vivo and thereby having a good therapeutic potential on TNBC. Taken together, these results suggest that 3r may be a novel Fam20C inhibitor with anti-proliferative and apoptosis-inducing activities, which would shed light on discovering more small-molecule drugs for the future TNBC therapy.
Novel CDK2 inhibitor and application thereof in resisting of breast cancer
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Paragraph 0041; 0045; 0049, (2018/05/16)
The invention relates to a CDK2 inhibitor and application thereof, belonging to the technical field of anti-tumor pharmacy. The invention provides a compound as the CDK2 inhibitor. The compound contains a compound represented by a formula (shown in the de
POTASSIUM CHANNEL MODULATORS
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Paragraph 0285-0286, (2018/01/14)
Provided are novel compounds of Formula (I): and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with potassium channels. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I), pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with potassium channels.
HEPATITIS B VIRAL ASSEMBLY EFFECTORS
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Paragraph 00282, (2016/10/31)
Novel assembly effector compounds having a therapeutic effect against hepatitis B viral (HBV) infection are disclosed. Assembly effector molecules described herein can lead to defective viral assembly and also may affect other viral activities associated with chronic HBV infection. Also disclosed is a process to synthesize disclosed compounds, method of treatment of HBV by administration of disclosed compounds, and use of these compounds in the manufacture of medicaments against HBV.
Synthesis, antimalarial activity, heme binding and docking studies of 4-aminoquinoline-pyrimidine based molecular hybrids
Kumar, Deepak,Khan, Shabana I.,Tekwani, Babu L.,Ponnan, Prija,Rawat, Diwan S.
, p. 63655 - 63669 (2015/02/19)
A series of novel 4-aminoquinoline-pyrimidine hybrids was synthesized and evaluated for their antimalarial activity. Several compounds showed potent antimalarial activity against both CQ-sensitive and CQ-resistant strains of P. falciparum with no cytotoxi
Synthesis of piperazine tethered 4-aminoquinoline-pyrimidine hybrids as potent antimalarial agents
Thakur, Anuj,Khan, Shabana I.,Rawat, Diwan S.
, p. 20729 - 20736 (2014/06/09)
A series of 4-aminoquinoline-pyrimidine hybrids linked through piperazine were synthesized and evaluated for their in vitro antimalarial activity against chloroquine (CQ)-sensitive and chloroquine (CQ)-resistant strains of Plasmodium falciparum and cytoto
