80199-93-5Relevant academic research and scientific papers
Development of new HO-1 inhibitors by a thorough scaffold-hopping analysis
Floresta, Giuseppe,Pittalà, Valeria,Sorrenti, Valeria,Romeo, Giuseppe,Salerno, Loredana,Rescifina, Antonio
, p. 334 - 339 (2018/10/05)
HO-1 inhibition is considered a valuable anticancer approach. In fact, up-regulation of HO-1 had been repeatedly reported in many types of human malignancies, and in these clinical cases, poor outcomes are reported. To identify novel HO-1 inhibitors suitable for drug development, a scaffold-hopping strategy calculation was utilized to design novel derivatives. Different parts of the selected molecule were analyzed and the different series of novel compounds were virtually evaluated. The calculation for the linker moiety of the classical HO-1 inhibitors structure led us to compounds 5 and 6. A synthetic pathway for the two molecules was designed and the compounds were synthesized. The biological activity revealed an HO-1 inhibition of 0.9 and 54 μM for molecules 5 and 6 respectively. This study suggested that our scaffold-hopping approach was successful and these results are ongoing for further development.
β1-Selective Adrenoceptor Antagonists. 3. 4-Azolyl-Linked Phenoxypropanolamines
Machin, Peter J.,Hurst, David N.,Bradshaw, Rachel M.,Blaber, Leslie C.,Burden, David T.,Melarange, Rosemary A.
, p. 503 - 509 (2007/10/02)
A series of 4-substituted phenoxypropanolamines has been prepared and examined for β-adrenoceptor activity.The 4-substituents, di- and triazole ring systems connected to the phenoxy ring by different length chains, were chosen as a means of introducing ca
