491867-63-1

Upstream product

• 90-02-8 salicylaldehyde 
• 100-83-4 meta-hydroxybenzaldehyde 
• 105-56-6 ethyl 2-cyanoacetate 

Downstream Products

• 1270172-42-3 4-amino-2-(3-(2-(4-methylpiperazin-1-yl)ethoxy)phenyl)-5H-chromeno[4,3-d]pyrimidin-5-one 
• 1306753-84-3 4-amino-2-(3-(3-(pyrrolidin-1-yl)propoxy)phenyl)-5H-chromeno[4,3-d]pyrimidin-5-one 
• 1270172-43-4 4-amino-2-(3-(3-(4-methylpiperazin-1-yl)propoxy)phenyl)-5H-chromeno[4,3-d]pyrimidin-5-one 
• 1270172-72-9 4-amino-2-(3-(2-bromoethoxy)phenyl)-5H-chromeno[4,3-d]pyrimidin-5-one 
• 1270172-74-1 4-amino-2-(3-(3-bromopropoxy)phenyl)-5H-chromeno[4,3-d]pyrimidin-5-one 

Relevant academic research and scientific papers

Design and synthesis of 2-phenylpyrimidine coumarin derivatives as anticancer agents

A series of 2-phenylpyrimidine coumarin derivatives with potential telomerase-inhibiting activity was designed and synthesized. All of the compounds were screened for antiproliferative activity against CNE2, KB, and Cal27 cell lines in vitro. The results showed that most of the derivatives had a favorable effect on resisting tumor cell proliferation; compound 13, 3-(4-amino-5-oxo-5H-chromeno[4,3-d]pyrimidin-2-yl)phenyl 4-(dimethylamino)benzenesulfonate, exhibited the best activity. Flow cytometry revealed that compound 13 can inhibit CNE2 proliferation. Telomerase inhibition and in vitro antitumor activity were consistent among the compounds, but compound 13 showed the best telomerase-inhibiting activity and could inhibit telomere extension. Molecular docking results indicated that compound 13 bonded with telomerase reverse transcriptase (TERT) through multiple interactions, including hydrogen bonding and hydrophobic interactions. The results of the study provide further information on 2-phenylpyrimidine coumarins, expanding the types of telomerase inhibitors as the parent structures.

Disubstituted 2-phenyl-benzopyranopyrimidine derivatives as a new type of highly selective ligands for telomeric G-quadruplex DNA

A series of 2-phenyl-benzopyranopyrimidine (PBPP) derivatives with alkylamino side chains were synthesized and found to be a new type of highly selective ligand to bind with telomeric G-quadruplex DNA, and their biological properties were reported for the first time. Their interactions with telomeric G-quadruplex DNA were studied with FRET melting, surface plasmon resonance, CD spectroscopy, and molecular modeling. Our results showed that the disubstituted PBPP derivatives could strongly bind to and effectively stabilize the telomeric G-quadruplex structure, and had significant selectivity for G-quadruplex over duplex DNA. In comparison, the mono substituted derivatives had much less effect on the G-quadruplex, suggesting that the disubstitution of PBPP is essential for its interaction with the G-quadruplex. Furthermore, telomerase inhibition of the PBPP derivatives and their cellular effects were studied, and compound 11b was found to be the most promising compound as a telomerase inhibitor and telomeric G-quadruplex binding ligand for further development for cancer treatment.