- Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies
-
Concurrent inhibition of Janus kinase (JAK) and histone deacetylase (HDAC) could potentially improve the efficacy of the HDAC inhibitors in the treatment of cancers and resolve the problem of HDAC inhibitor resistance in some tumors. Here, a novel series
- Liang, Xuewu,Zang, Jie,Li, Xiaoyang,Tang, Shuai,Huang, Min,Geng, Meiyu,Chou, C. James,Li, Chunpu,Cao, Yichun,Xu, Wenfang,Liu, Hong,Zhang, Yingjie
-
p. 3898 - 3923
(2019/04/25)
-
- Novel CDK2 inhibitor and application thereof in resisting of breast cancer
-
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
- -
-
Paragraph 0041; 0042; 0046
(2018/05/16)
-
- Design, synthesis and biological evaluation of pyrimidine derivatives as novel CDK2 inhibitors that induce apoptosis and cell cycle arrest in breast cancer cells
-
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
- Wang, Yiting,Chen, Yanmei,Cheng, Xiaoling,Zhang, Ke,Wang, Hangyu,Liu, Bo,Wang, Jinhui
-
p. 3491 - 3501
(2018/05/31)
-
- Pyrimidine compound, EGFR inhibitor and application of EGFR inhibitor
-
The invention discloses a pyrimidine compound, an EGFR inhibitor and application of the EGFR inhibitor. The pyrimidine compound is prepared from a compound shown in the formula I or pharmaceutically acceptable salt thereof, a stereoisomer, and a solvate or prodrug. The EGFR inhibitor contains the pyrimidine compound. The pyrimidine compound can inhibit activated or resistant mutation of one or more kinds of EGFRs, can inhibit proliferation of the EGFR T790M/L858R double-mutant enzyme in the nanomolar concentration, but has a weak inhibiting effect on the wild EGFR enzyme; the pyrimidine compound is applicable to treatment of the EGFR-sensitive mutations cancer and also suitable for cases with secondary dug resistance in present EGFR-TKI treatment; meanwhile, toxic and side effects caused by inhibition on the wild EGFR are greatly reduced due to the mutation selectivity of the pyrimidine compound, and the pyrimidine compound is an ideal treatment drug for diseases caused by EGFR mutation.
- -
-
Paragraph 0080; 0081; 0082
(2017/04/28)
-
- 4-Aminoquinoline-Pyrimidine hybrids: Synthesis, antimalarial activity, heme binding and docking studies
-
A series of novel 4-aminoquinoline-pyrimidine hybrids has been synthesized and evaluated for their antimalarial activity. Several compounds showed promising in vitro antimalarial activity against both CQ-sensitive and CQ-resistant strains with high select
- Kumar, Deepak,Khan, Shabana I.,Tekwani, Babu L.,Ponnan, Prija,Rawat, Diwan S.
-
p. 490 - 502
(2014/12/11)
-
- Synthesis of piperazine tethered 4-aminoquinoline-pyrimidine hybrids as potent antimalarial agents
-
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
- Thakur, Anuj,Khan, Shabana I.,Rawat, Diwan S.
-
p. 20729 - 20736
(2014/06/09)
-
- N,N'-2,4-DIANILINOPYRIMIDINE DERIVATIVES, PREPARATION THEREOF AS DRUGS, PHARMACEUTICAL COMPOSITIONS ESSENTIALLY AS IKK INHIBITORS
-
The disclosure relates to a compound of formula (I): wherein R, R1, R2, R3, R4, R5, R6 and Z are as defined in the specification, to compositions containing them, to processes for preparing them, and to their use in the treatment or prevention of conditio
- -
-
Page/Page column 14
(2010/04/30)
-
- Novel 2,4-Dianilinopyrimidine Derivatives, the Preparation Thereof, Their Use as Medicaments, Pharmaceutical Compositions and, in Particular, as IKK Inhibitors
-
The disclosure relates to compounds of formula (I): wherein R1-R5, A and Y are as defined in the disclosure, to compositions comprising said compounds, and to processes for making and methods of using the same.
- -
-
Page/Page column 22-23
(2008/12/04)
-
- Development of N-2,4-pyrimidine-N-phenyl-N′-phenyl ureas as inhibitors of tumor necrosis factor alpha (TNF-α) synthesis. Part 1
-
A new class of tumor necrosis factor alpha (TNF-α) synthesis inhibitors based on an N-2,4-pyrimidine-N-phenyl-N′-phenyl urea scaffold is described. Many of these compounds showed low-nanomolar activity against lipopolysaccharide stimulated TNF-α productio
- Brugel, Todd A.,Maier, Jennifer A.,Clark, Michael P.,Sabat, Mark,Golebiowski, Adam,Bookland, Roger G.,Laufersweiler, Matthew J.,Laughlin, Steven K.,VanRens, John C.,De, Biswanath,Hsieh, Lily C.,Mekel, Marlene J.,Janusz, Michael J.
-
p. 3510 - 3513
(2007/10/03)
-
- Development of N-2,4-pyrimidine-N-phenyl-N′-alkyl ureas as orally active inhibitors of tumor necrosis factor alpha (TNF-α) synthesis. Part 2
-
A new class of tumor necrosis factor alpha (TNF-α) synthesis inhibitors based on a N-2,4-pyrimidine-N-phenyl-N′-alkyl urea scaffold is described. Many of these compounds showed low-nanomolar activity against lipopolysaccharide stimulated TNF-α production.
- Maier, Jennifer A.,Brugel, Todd A.,Clark, Michael P.,Sabat, Mark,Golebiowski, Adam,Bookland, Roger G.,Laufersweiler, Matthew J.,Laughlin, Steven K.,VanRens, John C.,De, Biswanath,Hsieh, Lily C.,Brown, Kimberly K.,Juergens, Karen,Walter, Richard L.,Janusz, Michael J.
-
p. 3514 - 3518
(2008/09/20)
-
- Tri-substituted ureas as cytokine inhibitors
-
The present invention relates to 1,1,3-tri-substituted ureas which inhibit the extracellular release of inflammatory cytokines, said cytokines responsible for one or more human or higher mammalian disease states. The present invention further relates to c
- -
-
Page/Page column 7
(2010/02/14)
-