82789-32-0Relevant articles and documents
Novel β-carboline-based indole-4,7-quinone derivatives as NAD(P)H: Quinone-oxidoreductase-1 inhibitor with potent antitumor activities by inducing reactive oxygen species, apoptosis, and DNA damage
Guo, Yibing,Xu, Liancheng,Ling, Changchun,Yang, Tao,Zheng, Wenjie,Lv, Jin,Guo, Qingsong,Chen, Bohua
, p. 1433 - 1446 (2020/07/13)
Eighteen new β-carboline-based indole-4,7-quinone derivatives (12a–i and 13a–i) were designed and synthesized, and their in vitro and in vivo antiproliferative activities were studied. Most of target compounds showed strong inhibition on three human tumor cells' proliferation. In particular, the most active compound 13g not only displayed more prominent antiproliferative activities than β-lapachone, a clinical antitumor candidate, but also exerted significant NAD(P)H: quinone-oxidoreductase-1 (NQO1) inhibitory activity and NQO1-dependent cytotoxicity in HT29 cells. Furthermore, 13g dose-dependently induced high ROS levels in HT29 cells, and selectively inhibited cancer cell but not non-tumor colon cell proliferation in vitro. Importantly, 13g promoted HT29 cell apoptosis and DNA damage by regulating relative apoptotic proteins and H2AX expression. Finally, 13g displayed significant growth inhibition of HT29 human colorectal adenocarcinoma xenograft in mice without overt toxicity.
Syntheses of new substituted triazino tetrahydroisoquinolines and β-carbolines as novel antileishmanial agents
Kumar, Arun,Katiyar, Sanjay Babu,Gupta, Suman,Chauhan, Prem M.S.
, p. 106 - 113 (2007/10/03)
A series of triazino tetrahydroisoquinolines (3-5) and β-carboline derivatives (15-27) have been synthesized as novel antileishmanial agents. Among them, compounds 15, 16 and 25 have shown 78.0%, 78.6% and 68.0% in vivo inhibition against Leishmania donov
Potent 1,3-disubstituted-9H-pyrido[3,4-b]indoles as new lead compounds in antifilarial chemotherapy
Srivastava, Sanjay K.,Agarwal, Alka,Chauhan, Prem M. S.,Agarwal, Shiv K.,Bhaduri, Amiya P.,Singh, Som N.,Fatima, Nigar,Chatterjee, Ranjit K.
, p. 1667 - 1672 (2007/10/03)
Substituted 9H-pyrido[3,4-b]indoles (β-carbolines), identified in our laboratory as potential pharmacophores for designing macrofilaricidal agents, have been explored further for identifying the pharmacophore responsible for the high order of adulticidal