A new application about 151266-23-8

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions. you can also check out more blogs about 151266-23-8. Formula: C5H4IN5.

Chemistry, like all the natural sciences, Formula: C5H4IN5, begins with the direct observation of nature¡ª in this case, of matter.151266-23-8, Name is 3-Iodo-1H-pyrazolo[3,4-d]pyrimidin-4-amine, SMILES is NC1=C2C(NN=C2I)=NC=N1, belongs to pyrimidines compound. In a document, author is Xiang, Weiguo, introduce the new discover.

The 3-D conformational shape of N-naphthyl-cyclopenta[d]pyrimidines affects their potency as microtubule targeting agents and their antitumor activity

A series of methoxy naphthyl substituted cyclopenta [d]pyrimidine compounds, 4-10, were designed and synthesized to study the influence of the 3-D conformation on microtubule depolymerizing and antiproliferative activities. NOESY studies with the N,2-dimethyl N-(6′-methoxynaphthyl-1′-amino)-cyclopenta [d]pyrimidin-4-amine (4) showed hindered rotation of the naphthyl ring around the cyclopenta[d]pyrimidine scaffold. In contrast, NOESY studies with N,2-dimethyl-N-(5′-methoxynaphthyl-2′-amino)-cyclopenta[d]pyrimidin-4-amine (5) showed free rotation of the naphthyl ring around the cyclopenta[d]pyrimidine scaffold. The rotational flexibility and conformational dissimilarity between 4 and 5 led to a significant difference in biological activities. Compound 4 is inactive while 5 is the most potent in this series with potent microtubule depolymerizing effects and low nanomolar IC50 values in vitro against a variety of cancer cell lines. The ability of 5 to inhibit tumor growth in vivo was investigated in a U251 glioma xenograft model. The results show that 5 had better antitumor effects than the positive control temozolomide and have identified 5 as a potential preclinical candidate for further studies. The influence of conformation on the micmtubule depolymerizing and antitumor activity forms the basis for the development of conformation-activity relationships for the cyclopenta [d] pyrimidine class of microtubule targeting agents.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions. you can also check out more blogs about 151266-23-8. Formula: C5H4IN5.

Reference:
Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia