Synthesis and Biological Evaluation of New Selective Cytotoxic Cyclolignans Derived from Podophyllotoxin was written by Castro, Maria Angeles;del Corral, Jose Maria Miguel;Gordaliza, Marina;Garcia, Pablo A.;Gomez-Zurita, Maria Antonia;Garcia-Gravalos, Maria Dolores;de la Iglesia-Vicente, Janis;Gajate, Consuelo;An, Feiyun;Mollinedo, Faustino;San Feliciano, Arturo. And the article was included in Journal of Medicinal Chemistry in 2004.Recommanded Product: 1-Ethyl-1H-pyrazol-5-amine This article mentions the following:
Podophyllotoxin and some of its derivatives are cyclolignans currently used for removing warts and in the clin. treatment of malign neoplasms. As such, they were an objective of the scientific community for decades, in the search for more potent and more selective anticancer agents. Interest in the chemoinduction of drug selectivity led to the design and preparation of new podophyllotoxin derivatives by reaction of podophyllic aldehyde with aliphatic, aromatic, and heteroaromatic amines. Several of the resulting imines displayed a significant selectivity against human colon carcinoma cells, even higher than that of the starting aldehyde. Addnl. biol. studies indicate that these derivatives induce microtubule depolymerization, arrest cells at the G2/M phase of cell cycle, and are able to induce a delayed apoptosis after 48 h of treatment, characterized by caspase-3 activation. In the experiment, the researchers used many compounds, for example, 1-Ethyl-1H-pyrazol-5-amine (cas: 3528-58-3Recommanded Product: 1-Ethyl-1H-pyrazol-5-amine).
1-Ethyl-1H-pyrazol-5-amine (cas: 3528-58-3) belongs to pyrazole derivatives. Pyrazole has two ring nitrogen atoms in which N1 is pyrrolic and N2 is pyridine-like. The N1 nitrogen is not reactive but is deprotonated in the presence of a base-forming anion. Protonation of pyrazole in strong acid leads to pyrazolium cations, which undergo electrophilic substitution preferentially at C3 rather than C4. The pyrazole anion is not reactive toward nucleophiles but is mostly reactive to electrophiles.Recommanded Product: 1-Ethyl-1H-pyrazol-5-amine
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics