203436-45-7Relevant articles and documents
A Stepwise Approach for the Synthesis of Folic Acid Conjugates with Protein Kinase Inhibitors
Kraj?ovi?ová, Soňa,Gucky, Tomá?,Hendrychová, Denisa,Kry?tof, Vladimír,Soural, Miroslav
, p. 13530 - 13541 (2017)
Herein, we report an alternative synthetic approach for selected 2,6,9-trisubstituted purine CDK inhibitor conjugates with folic acid as a drug-delivery system targeting folate receptors. In contrast to the previously reported approaches, the desired conj
Design, synthesis and biological evaluation of a novel tubulin inhibitor SKLB0565 targeting the colchicine binding site
Feng, Zhanzhan,Hu, Xi,Li, Lu,Wang, Qianqian,Xia, Yong,Xu, Ying,Yu, Luoting,Zhang, Qiangsheng
, (2020)
A series of 3-(((9H-purin-6-yl) amino) methyl) pyridin-2(1H)-one derivatives were designed, synthesized and confirmed as tubulin polymerization inhibitors. All compounds were evaluated for their anti-proliferative activities on three colorectal carcinoma (CRC) cell lines. Among these compounds, SKLB0565 displayed noteworthy potency against eight CRC cell lines with IC50 values ranging from 0.012 μM and 0.081 μM. Besides, SKLB0565 inhibited tubulin polymerization, caused G2/M phase cell cycle arrest, depolarized mitochondria and induced cell apoptosis in CRC cells. Furthermore, SKLB0565 suppressed cell migration and disrupted the capillary tube formation of human umbilical vein endothelial cells (HUVECs). Our data clarified that SKLB0565 is a promising anti-tubulin agent for CRC therapy which is worthy of further evaluation.
PROCESS FOR THE PREPARATION OF PURINE DERIVATIVES EXHIBITING CDK INHIBITORY ACTIVITY
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Page/Page column 38, (2021/07/31)
The present invention relates to a process for preparing a compound of formula [I], or a pharmaceutically acceptable salt thereof, said process comprising the steps of: (i) forming a reaction mixture comprising a compound of formula [II] and a compound of formula [III]; (ii) heating said reaction mixture to a temperature of at least about 130°C to form a compound of formula [I]; (iii) isolating said compound of formula [I] from the mixture and optionally recovering unreacted compound of formula [III]; and (iv) optionally converting said compound of formula [I] into salt form; wherein: R1 and R2 are each independently H, alkyl or haloalkyl; R3 and R4 are each independently H, alkyl, haloalkyl or aryl; R5 is alkyl, alkenyl, cycloalkyl or cycloalkyl-alkyl, each of which may be optionally substituted with one or more OH groups; R6 is selected from cyclopropylamino, cyclopropylmethylamino, cyclobutylamino, cyclobutylmethylamino and where one of X, Y and Z is N and the remainder are CR9; R7, R8 and each R9 are independently H, alkyl or haloalkyl, wherein at least one of R7, R8 and R9 is other than H. Further aspects of the invention relate to a process for preparing intermediates of formula [II], and other intermediates useful in the synthesis of compounds of formula [I].
AROMATIC COMPOUNDS FOR USE IN ACTIVATING HEMATOPOIETIC STEM AND PROGENITOR CELLS
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Paragraph 0251, (2020/06/19)
Disclosed herein are new aromatic compounds, compositions that include one or more aromatic compounds, and methods of synthesizing the same. Also disclosed herein are methods of increasing and/or expanding cells, including stem cells, hematopoietic stem cells, progenitor cells, and placenta or cord blood-derived cells, with one or more compounds or compositions described herein. Also disclosed herein are methods of increasing and/or expanding differentiated hematopoietic cells with one or more compounds or compositions described herein.
