90065-71-7Relevant academic research and scientific papers
Novel pyrrolopyrimidine derivatives induce p53-independent apoptosis via the mitochondrial pathway in colon cancer cells
Aka, Yeliz,Kilic-Kurt, Zühal,Kutuk, Ozgur
, (2020/09/11)
A series of novel pyrrolopyrimidine urea derivatives were synthesized and evaluated for their anticancer activity against colon cancer cell lines. Compounds showed the remarkable cytotoxic activity on HCT-116 wt cell line. The most potent compound 4c (IC50 = 0.14 μM) induced apoptosis in HCT-116 wt and HCT-116 p53?/? cell lines. Otherwise, treatment of HCT-116 BAX?/?BAK?/? cells with compound 4c didn't lead to activation of apoptosis, suggesting that compound 4c induces apoptotic cell death by activating BAX/BAK-dependent pathway. Moreover, while the compound 4c increase the activation of caspase-3 and caspase-9 levels in HCT-116 wt and HCT-116 p53?/? cells, caspase-3 or caspase-9 activation was not observed in HCT-116 BAX?/?BAK?/? cells. In addition, compound 4c induced mitochondrial apoptosis in cells grown as oncospheroids, which better mimic the in vivo milieu of tumors. 4c treatment also activated JNK along with inhibition of prosurvival kinases such as Akt and ERK 1/2 in HCT-116 wt and HCT-116 p53 ?/? cells as well as in HCT-116 BAX?/?BAK?/? cells. Notably, our results indicated that compound 4c induced mitochondrial apoptosis through activation p53-independent apoptotic signaling pathways.
Design, synthesis and in vitro apoptotic mechanism of novel pyrrolopyrimidine derivatives
Kilic-Kurt, Zühal,Bakar-Ates, Filiz,Aka, Yeliz,Kutuk, Ozgur
, p. 511 - 519 (2018/11/24)
In this work we described the synthesis and evaluation of cytotoxic and apoptotic activity of novel pyrrolopyrimidine derivatives against A549, PC3 and MCF-7 cells. Among the synthesized compounds, 6b, 8a, 9a and 7a, 8b displayed the significant cytotoxic
The synthesis and determination of acidic ionization constants of certain 5-substituted 2-aminopyrrolo[2,3-d]pyrimidin-4-ones and methylated analogs
Hoops, Geoffrey C.,Park, Julie,Garcia, George A.,Townsend, Leroy B.
, p. 767 - 781 (2007/10/03)
The acidic ionization constants were determined for a series of 5-substituted 2-aminopyrrolo[2,3-dl-pyrimidin-4-ones and N-3- and N-7-methylated analogs thereof. The syntheses of the methylated analogs are also described.
Isomeric N-methyl-7-deazaguanines: Synthesis, structural assignment, and inhibitory activity on xanthine oxidase
Seela,Bussmann,Gotze,Rosemeyer
, p. 981 - 985 (2007/10/02)
The N-methyl isomers of 2-amino-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one1 (2a) have been synthesized regiospecifically and their structures assigned. The 3-methyl thylcompound was obtained by alkylation of the parent chromophore 2a with dim
