362619-79-2Relevant academic research and scientific papers
Synthesis and growth-inhibitory activities of imidazo?5,1-d]-1,2,3,5-tetrazine-8-carboxamides related to the anti-tumour drug temozolomide, with appended silicon, benzyl and heteromethyl groups at the 3-position
Cousin, David,Hummersone, Marc G.,Bradshaw, Tracey D.,Zhang, Jihong,Moody, Christopher J.,Foreiter, Magdalena B.,Summers, Helen S.,Lewis, William,Wheelhouse, Richard T.,Stevens, Malcolm F.G.
supporting information, p. 545 - 553 (2018/03/28)
A series of 3-(benzyl-substituted)-imidazo?5,1-d]-1,2,3,5-tetrazines (13) and related derivatives with 3-heteromethyl groups has been synthesised and screened for growth-inhibitory activity in vitro against two pairs of glioma cell lines with temozolomide-sensitive and -resistant phenotypes dependent on the absence/presence of the DNA repair protein O6-methylguanine-DNA methyltransferase (MGMT). In general the compounds had low inhibitory activity with GI50 values >50 μM against both sets of cell lines. Two silicon-containing derivatives, the TMS-methylimidazotetrazine (9) and the SEM-analogue (10), showed interesting differences: compound (9) had a profile very similar to that of temozolomide with the MGMT+ cell lines being 5 to 10-fold more resistant than MGMT- isogenic partners; the SEM-substituted compound (10) showed potency across all cell lines irrespective of their MGMT status.
Design and synthesis of small chemical inhibitors containing different scaffolds for lck SH2 domain
Park, See-Hyoung,Kang, Sun-Hee,Lim, Sang-Hyeong,Oh, Hyun-Sik,Lee, Keun-Hyeung
, p. 3455 - 3459 (2007/10/03)
On the basis of the structure of (R)-rosmarinic acid, a series of small chemical compounds with a different scaffold was synthesized as inhibitors for lck SH2 domain. From ELISA results, most of all chemical compounds showed a similar or a little lower bi
