83393-46-8Relevant articles and documents
Synthesis and evaluation of C3 substituted chalcone-based derivatives of 7-azaindole as protein kinase inhibitors
Qhobosheane, Malikotsi A.,Legoabe, Lesetja J.,Josselin, Béatrice,Bach, Stéphane,Ruchaud, Sandrine,Beteck, Richard M.
, p. 1395 - 1407 (2020)
Chalcones are a group of naturally occurring or synthetic compounds which possess a wide range of biological activities. In this paper, a series of twenty-three 7-azaindole-chalcone hybrids (5a–w) were synthesized and evaluated as potential protein kinase inhibitors. Analyses of structure–activity relationships revealed that some of these compounds exhibit significant activity against Haspin kinase, with compounds 5f and 5q exhibiting IC50 values of 0.47 and 0.41?μM, respectively. Furthermore, 5f also inhibits cyclin-dependent kinase 9 (CDK9/CyclinT) in a micromolar potency (IC50?=?2.26?μM). This novel dual-target inhibitor is a promising lead for the development of chemopreventive/chemotherapeutic agents.
Discovery of novel 4-azaaryl-N-phenylpyrimidin-2-amine derivatives as potent and selective FLT3 inhibitors for acute myeloid leukaemia with FLT3 mutations
Long, Yi,Yu, Mingfeng,Ochnik, Aleksandra M.,Karanjia, Jasmine D.,Basnet, Sunita KC.,Kebede, Alemwork A.,Kou, Lianmeng,Wang, Shudong
, (2021/02/03)
Feline McDonough sarcoma (FMS)-like tyrosine kinase 3 (FLT3) is one of the most pursued targets in the treatment of acute myeloid leukaemia (AML) as its gene amplification and mutations, particularly internal tandem duplication (ITD), contribute to the pa
Double (amino-sulfur generation of formic acid ) - 1,3-propane diester compound and its synthetic method, pharmaceutical composition and use thereof
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Paragraph 0296-0299, (2016/10/08)
The invention relates to a bis(aminodithioformate)-1,3-propane diester compound, and synthesis method thereof, a pharmaceutical composition containing the compound and a use, and especially relates to the use in preparing drugs for treating or preventing cancers. The compound is represented as the formula (I), wherein A is selected from substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heterocyclic group, R1 and R2 are the same or different and are independently selected from hydrogen, alkyl, aryl alkyl or heteroaryl alkyl, or a substituted or unsubstituted heterocyclic ring formed together by the R1, the R2 and an N atom connected with the R1 and the R2.