59898-53-2Relevant academic research and scientific papers
Facile synthesis of autophagonizer and evaluation of its activity to induce autophagic cell death in apoptosis-defective cell line
Nguyen, Jennifer,Chen, Luxi,Kumar, Dhiraj,Lee, Jiyong
, p. 4753 - 4756 (2016/09/13)
Some cancer cells are resistant to apoptosis, rendering them irresponsive towards apoptosis-inducing chemotherapy drugs. Another mode of action to kill these apoptosis-defective cells is essential and autophagy, a dynamic process that degrades cytoplasmic contents for cellular maintenance, has been considered as one of the alternate routes. A small molecule inducer of autophagy, autophagonizer was reported to induce cell death through a novel process that is independent of extrinsic apoptosis and the normal signaling pathways of autophagy. Here, we describe an efficient synthetic procedure for the autophagonizer. The newly synthesized autophagonizer (DK-1-49) resulted in an accumulation of autophagy-associated LC3-II and enhanced levels of autophagosomes and acidic vacuoles. Furthermore, cell viability was inhibited by autophagic cell death in not only human cancer cells but also Bax/Bak double-knockout cells. These findings highlight that intrinsic apoptosis is not also involved in the induction of cellular death by the autophagonizer suggesting the autophagonizer is a promising candidate for anticancer therapeutics for cancer cells that are resistant to apoptosis-inducing chemotherapy.
Synthesis and transformations of 3-ethoxycarbonyl-2-(N-R-thioreido)thiophenes
Chumakova,Demchenko,Krasovsky,Dolishnyak,Lozinskii
, p. 1002 - 1012 (2007/10/03)
3-Ethoxycarbonyl-2-N-R-thioureido)-4,5,6,7-tetrahydrobenzo[b]thiophenes were obtained by the reaction of 2- amino-3-ethoxycarbonyl-4,5,6,7-tetrahydrobenzo[b]thiophene with isothiocyanates and of 3-ethoxycarbonyl-2-isothiocyanato-4,5,6,7-tetrahydrobenzo[b]
Synthesis of 3 substituted thieno[2,3 d]pyrimidin 4(3H) one 2 mercaptoacetic acids and their ethyl esters for pharmacological screening
Devani,Shishoo,Pathak,Parikh,Shah,Padhya
, p. 660 - 664 (2007/10/08)
3 Substituted thieno[2,3 d]pyrimidin 4(3H) one 2 mercaptoacetic acids and their ethyl esters were synthesized from 2 mercaptothieno[2,3 d]pyrimidin 4 (3H) ones, which were obtained by cyclization of thienylthioureas in acidic medium. Analgesic, anti inflammatory, and anticonvulsant activities were found in some of these compounds. Significant antimicrobial activity was exhibited by thienylthioureas.
