37787-77-2Relevant articles and documents
Design, synthesis and biological evaluation of new bivalent quinazoline analogues as IAP antagonists
Bae, Inhwan,Kim, Daejin,Choi, Jaeyul,Kim, Jisook,Kim, Minjeong,Park, Bokyung,Kim, Young Hoon,Ahn, Young Gil,Hyung Kim, Ha,Kim, Dae Kyong
supporting information, (2021/01/26)
We recently reported the biological evaluations of monovalent IAP antagonist 7 with good potency (MDA-MB-231, IC50 = 19 nM). In an effort to increase cellular activity and improve favorable drug-like properties, we newly designed and synthesized bivalent analogues based on quinazoline structure of 7. Optimization of cellular potency and CYP inhibition led to the identification of 27, which showed dramatic increase of over 100-fold (IC50 = 0.14 nM) and caused substantial tumor regressions in MDA-MB-231 xenograft model. These results strongly support 27 as a promising bivalent antagonist for the development of an effective anti-tumor approaches.
Modular Synthesis of Carbazole-Substituted Phthalimides as Potential Photocatalysts
F?ldesi, Tamás,Gonda, Zsombor,Nagy, Bálint,Novák, Zoltán
supporting information, (2021/11/22)
The modular synthesis of carbazole functionalized phthalimides (PIs) and their applicability as catalyst in selected photocatalytic transformations are reported. The developed synthetic approach provides high variability of phthalimide considering that the synthesis of the phthalimide core can be easily performed. Starting from fluorophthalic acid anhydrides, the corresponding fluorophthalimides were prepared with various amines, and the fluoro function ensured the introduction of carbazoles into the phthalimide framework through aromatic nucleophilic substitution. Besides the synthetic developments, some of the carbazolyl phthalimides were tested in four different photocatalytic transformations, which showed attractive and comparable activity to the known 4-CzIPN and noble metal complexes.
A Ni–Ir Dual Photocatalytic Liebeskind Coupling of Sulfonium Salts for the Synthesis of 2-Benzylpyrrolidines
Varga, Bálint,Gonda, Zsombor,Tóth, Balázs L.,Kotschy, András,Novák, Zoltán
, p. 1466 - 1471 (2019/11/03)
A new method has been developed for the synthesis of 2-benzylpyrrolidines utilizing cross-coupling and photoredox catalysis. Using a well-established dual Ni–Ir system, we were able to successfully couple benzylsulfonium salts with proline utilizing radical forming through CO2 extrusion. This enabled the simple one-step synthesis of 2-benzylpyrrolidines from stable, inexpensive starting materials.