139183-60-1Relevant articles and documents
New Spisulosine Derivative promotes robust autophagic response to cancer cells
Chaturvedi, Priyank,Datta, Dipak,Ganesher, Asha,Meena, Sanjeev,Mitra, Kalyan,Panda, Gautam,Sahai, Rohit
, (2020/01/13)
Therapy resistance by evasion of apoptosis is one of the hallmarks of human cancer. Therefore, restoration of cell death by non-apoptotic mechanisms is critical to successfully overcome therapy resistance in cancer. By rational drug design approach, here we try to provide evidence that subtle changes in the chemical structure of spisulosine completely switched its cytotoxic function from apoptosis to autophagy. Our most potent molecule (26b) in a series of 16 synthesized derivatives showed robust autophagic cell death in diverse cancer cells sparing normal counterpart. Compound 26b mediated lethal autophagy induction was confirmed by formation of characteristic autophagic vacuoles, LC3 puncta formation, upregulation of signature autophagy markers like Beclin and Atg family proteins. Altogether, we have detected novel autophagy inducer small molecule which can be tested further for drug discovery research.
Design and synthesis of fused tetrahydroisoquinoline-iminoimidazolines
Moas-Héloire, Valeria,Renault, Nicolas,Batalha, Vania,Arias, Angela Rincon,Marchivie, Mathieu,Yous, Said,Deguine, Noémie,Buée, Luc,Chavatte, Philippe,Blum, David,Lopes, Luisa,Melnyk, Patricia,Agouridas, Laurence
, p. 15 - 25 (2015/11/23)
In the aim of identifying new privileged structures, we describe the 5-steps synthesis of cyclic guanidine compounds "tetrahydroisoquinoline-iminoimidazolinesg" derived from tetrahydroisoquinoline-hydantoin core. In order to evaluate this new minimal structure and the impact of replacing a carbonyle by a guanidine moiety, their affinity towards adenosine receptor A2A was evaluated and compared to those of tetrahydroisoquinoline-hydantoin compounds.
A facile transformation of amino acids to functionalized coumarins
Bandyopadhyay, Anupam,Gopi, Hosahudya N.
scheme or table, p. 8089 - 8095 (2012/01/04)
The synthesis of novel chiral coumarins functionalized with proteinogenic amino acid side chains via N-protected γ-amino-β-keto esters and their incorporation into the cell permeable HIV-1 TAT peptide through the modified solid phase peptide synthesis are
