126728-20-9Relevant articles and documents
The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase
Malagu, Karine,Duggan, Heather,Menear, Keith,Hummersone, Marc,Gomez, Sylvie,Bailey, Christine,Edwards, Peter,Drzewiecki, Jan,Leroux, Frederic,Quesada, Mar Jimenez,Hermann, Gesine,Maine, Stephanie,Molyneaux, Carrie-Anne,Le Gall, Armelle,Pullen, James,Hickson, Ian,Smith, Lisa,Maguire, Sharon,Martin, Niall,Smith, Graeme,Pass, Martin
, p. 5950 - 5953 (2009)
We describe a novel series of potent inhibitors of the kinase activity of mTOR. The compounds display good selectivity relative to other PI3K-related kinase family members and, in cellular assays, inhibit both mTORC1 and mTORC2 complexes and exhibit good antiproliferative activity.
ION CHANNEL INHIBITOR COMPOUNDS FOR CANCER TREATMENT
-
, (2021/01/25)
The present invention concerns a compound of following general formula (I): where: either R is an R1 group and R′ is an -A1-Cy1 group, or R is an -A1-Cy1 group and R′ is an R1 group, R1 particularly being H or (C1-C6)alkyl group;A1 being an —NH— radical or —NH—CH2— radical;Cy1 particularly being a phenyl group,A is a fused (hetero)aromatic ring having 5 to 7 atoms, for use for treating cancer.
2,4-quinazolinediamine derivatives, and preparation method and application thereof
-
Paragraph 0211; 0214; 0215, (2017/04/18)
The invention discloses 2,4-quinazolinediamine derivatives, and a preparation method and application thereof, belonging to the field of medicines and preparation and application thereof. The 2,4-quinazolinediamine derivatives comprises compounds as shown in a formula (I) which is described in the specification and a solvate, hydrate, tautomer and pharmaceutically acceptable salt thereof. Test results show that the 2,4-quinazolinediamine derivatives have strong Wolbachia resisting activity; and in the derivatives, 2-isopropylamido substitution has good effect, and compounds with better Wolbachia resisting activity can be obtained by changing a 4-amido group. The compounds have activity in resisting plasmodia, Wolbachia and bacteria.