330551-06-9

Upstream product

• 10389-51-2 1-morpholino-4-nitrobenzene 
• 1414781-18-2 N⁴-cyclopentyl-N²-(4-morpholinophenyl)-5-nitropyrimidine-2,4-diamine hydrochloride 
• 1003-03-8 Cyclopentamine 
• 330550-92-0 2-chloro-N-cyclopentyl-5-nitropyrimidin-4-amine 

Downstream Products

• 1414781-27-3 C₂₆H₂₉N₇O 
• 330550-43-1 8-Cyclopentyl-2-[[4-(morpholin-4-yl)phenyl]amino]-8H-pteridin-7-one 
• 330550-44-2 8-Cyclopentyl-6-methyl-2-[[4-(morpholin-4-yl)phenyl]amino]-8H-pteridin-7-one 
• 330550-77-1 8-Cyclopentyl-2-[[4-(morpholin-4-yl]phenyl]amino]-5H,8H-pteridine-6,7-dione 

Relevant academic research and scientific papers

Design, synthesis and antiproliferative activity of novel 2,4-diamino-5-methyleneaminopyrimidine derivatives as potential anticancer agents

In order to discover new anticancer agents, 25 novel 2,4-diamino-5-methyleneaminopyrimidine derivatives were designed and synthesized based on our previous work via a ring-opening strategy. Among them, compared with 5-FU, compound 7i exhibited 4.9-, 2.9-,

Structural optimization and structure-activity relationships of N 2-(4-(4-methylpiperazin-1-yl)phenyl)- N 8-phenyl-9 H -purine-2,8-diamine derivatives, a new class of reversible kinase inhibitors targeting both EGFR-activating and resistance mutations

This paper describe the structural optimization of a hit compound, N 2-(4-(4-methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine- 2,8-diamine (1), which is a reversible kinase inhibitor targeting both EGFR-activating and drug-resistance (T790M) mutations but has poor binding affinity. Structure-activity relationship studies led to the identification of 9-cyclopentyl-N2-(4-(4-methylpiperazin-1-yl)phenyl)-N 8-phenyl-9H-purine-2,8-diamine (9e) that exhibits significant in vitro antitumor potency against the non-small-cell lung cancer (NSCLC) cell lines HCC827 and H1975, which harbor EGFR-activating and drug-resistance mutations, respectively. Compound 9e was further assessed for potency and selectivity in enzymatic assays and in vivo anti-NSCLC studies. The results indicated that compound 9e is a highly potent kinase inhibitor against both EGFR-activating and resistance mutations and has good kinase spectrum selectivity across the kinome. In vivo, oral administration of compound 9e at a dose of 5 mg/kg caused rapid and complete tumor regression in a HCC827 xenograft model, and an oral dose of 50 mg/kg initiated a considerable antitumor effect in an H1975 xenograft model.

Pteridinones as kinase inhibitors

Disclosed are compounds of Formulae (Ia), (Ib), (Ic), (Id) wherein: W is NH, S, SO, or SO2; R2 is (un)substituted aryl, (un)substituted heteroaryl, or (un)substituted carbocycle or heterocycle; Q is hydrogen or lower alkyl; R4