190973-17-2Relevant academic research and scientific papers
Identification of a new series of flavopiridol-like structures as kinase inhibitors with high cytotoxic potency
Alami, Mouad,Bach, Stéphane,Bignon, Jerome,Bonnet, Pascal,Brion, Jean-Daniel,Colas, Pierre,Hamze, Abdallah,Ibrahim, Nada,Josselin, Béatrice,Levaique, Helene,Messaoudi, Samir,Peyrat, Jean-Fran?ois,Robert, Thomas
, (2020/05/11)
In this work, unique flavopiridol analogs bearing thiosugars, amino acids and heterocyclic moieties tethered to the flavopiridol via thioether and amine bonds mainly on its C ring have been prepared. The analogs bearing thioether-benzimidazoles as substituents have demonstrated high cytotoxic activity in vitro against up to seven cancer cell lines. Their cytotoxic effects are comparable to those of flavopiridol. The most active compound 13c resulting from a structure-activity relationship (SAR) study and in silico docking showed the best antiproliferative activity and was more efficient than the reference compound. In addition, compound 13c showed significant nanomolar inhibition against CDK9, CDK10, and GSK3β protein kinases.
SUBSTITUTED AURONE ALKALOIDS AS ANTI-MYCOBACTERIAL AGENTS
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Page/Page column 10; 11, (2017/09/15)
The present invention relates to new generation of aurone alkaloid agents, their method of preparation and their use as drugs for treatment of tuberculosis.
Synthesis of newer piperidinyl chalcones and their anticancer activity in human cancer cell lines
Jayashree,Patel, Harshkumar H.,Mathew, Neethu Susan,Nayak, Yogendra
, p. 3673 - 3688 (2016/04/05)
Newer tetrahydropyridine chalcones were synthesized and tested for their antioxidant and anticancer activity. These molecules showed significant anticancer activity at IC50 50 μM in human cancer cell lines such as A549 (lung adenocarcinoma),
COMPOUNDS AND COMPOSITIONS COMPRISING CDK INHIBITORS AND METHODS FOR THE TREATMENT OF CANCER
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Page/Page column 31, (2010/11/18)
Disclosed herein are compounds suitable for use as antitumor agents, methods for treating cancer wherein the disclosed compounds are used in making a medicament for the treatment of cancer, methods for treating a tumor comprising, administering to a subject a composition comprising one or more of the disclosed cytotoxic agents, and methods for preparing the disclosed antitumor agents.
Bioactivity of glycogen phosphorylase inhibitors that bind to the purine nucleoside site
Hampson, Laura J.,Arden, Catherine,Agius, Loranne,Ganotidis, Minas,Kosmopoulou, Magda N.,Tiraidis, Costas,Elemes, Yiannis,Sakarellos, Constantinos,Leonidas, Demetres D.,Oikonomakos, Nikos G.
, p. 7835 - 7845 (2007/10/03)
The bioactivity in hepatocytes of glycogen phosphorylase inhibitors that bind to the active site, the allosteric activator site and the indole carboxamide site has been described. However, the pharmacological potential of the purine nucleoside inhibitor s
Novel 3-(4-oxo-4h-chromen-2-yl)-(1H)-quinolin-4-one derivatives, method for preparing same and pharmaceutical compositions containing same
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Page/Page column 6, (2008/06/13)
Compound of formula (I): wherein: R1, R2, R3, R4, R6, R8, R9 and R10, which may be the same or different, each represent a group selected from hydrogen, hydroxy, alkoxy, alkyl, arylalkoxy, alkoxycarbonylalkoxy and OR′ wherein R′ represents an ionised or ionisable group, R5 represents a group selected from alkyl, aryl and heteroaryl, R7 represents a group selected from hydrogen, hydroxy, alkoxy, alkyl and cycloalkyl, or R7 represents a nitrogen-containing or oxygen-containing heterocycle, its optical isomers, hydrates and solvates thereof and addition salts thereof, with a pharmaceutically acceptable acid or base. Medicinal products containing the same which are useful as anti-cancer agents.
Structure-activity relationship studies of flavopiridol analogues
Murthi, Krishna K.,Dubay, Marja,McClure, Christopher,Brizuela, Leonardo,Boisclair, Michael D.,Worland, Peter J.,Mansuri, Muzammil M.,Pal, Kollol
, p. 1037 - 1041 (2007/10/03)
Cyclin dependent kinases (CDKs) along with the complementary cyclins form key regulatory checkpoint controls on the cell cycle. Flavopiridol is a synthetic flavone that shows potent and selective cyclin-dependent kinase inhibitory activity. In this paper, we report modifications of the 3-hydroxy-1-methylpiperidinyl (D ring) of flavopiridol and their effect on CDK inhibitory activity. (C) 2000 Elsevier Science. All rights reserved.
