19007-49-9Relevant academic research and scientific papers
In vitro and in vivo anti-tumor activity of two gold(III) complexes with isoquinoline derivatives as ligands
Khan, Taj-Malook,Gul, Noor Shad,Lu, Xing,Wei, Jian-Hua,Liu, Yan-Cheng,Sun, Hongbin,Liang, Hong,Orvig, Chris,Chen, Zhen-Feng
, p. 333 - 343 (2019)
Two gold(III) complexes of isoquinoline derivatives: [Au(L1)Cl2] (Au1) and [Au(L2)Cl2] (Au2) have been prepared and characterized. Au1 and Au2 exhibited greater cytotoxicity than their corresponding ligands and
Rhodium(III) complexes with isoquinoline derivatives as potential anticancer agents:: In vitro and in vivo activity studies
Khan, Taj-Malook,Gul, Noor Shad,Lu, Xing,Kumar, Rajesh,Choudhary, Muhammad Iqbal,Liang, Hong,Chen, Zhen-Feng
, p. 11469 - 11479 (2019)
Two rhodium complexes Rh1 and Rh2 with isoquinoline derivatives were synthesized and characterized. Both complexes displayed strong anticancer activity against various cancer cells and low cytotoxicity against non-cancer cells. These complexes triggered a
New copper complexes inducing bimodal death through apoptosis and autophagy in A549 cancer cells
Chen, Ming,Chen, Zhen-Feng,Choudhary, Muhammad Iqbal,Gul, Noor Shad,Hou, Cheng,Huang, Ke-Bin,Khan, Taj-Malook,Liang, Hong
, (2020/10/12)
Two copper complexes, Cu1 (CuL1Cl2, L1 = 2-(6,7-dimethoxyisoquinolin-1-yl) aniline) and Cu2 (CuL2Cl2, L2 = 2-(6-methoxyisoquinolin-1-yl) aniline), were synthesized and characterized. These
Structural optimization of natural product nordihydroguaretic acid to discover novel analogues as AcrB inhibitors
Alenzy, Rawaf,Liu, Xingbang,Ma, Shutao,Ma, Yingang,Mowla, Rumana,Polyak, Steven W.,Song, Di,Teng, Yuetai,Venter, Henrietta,Wang, Yinhu
, (2019/12/24)
Drug efflux pumps confer multidrug resistance to dangerous bacterial pathogens which makes these proteins promising drug targets. Herein, we present initial chemical optimization and structure-activity relationship (SAR) data around a previously described efflux pump inhibitor, nordihydroguaretic acid (NDGA). Four series of novel NDGA analogues that target Escherichia coli AcrB were designed, synthesized and evaluated for their ability to potentiate the activity of antibiotics, to inhibit AcrB-mediated substrate efflux and reduce off-target activity. Nine novel structures were identified that increased the efficacy of a panel of antibiotics, inhibited drug efflux and reduced permeabilization of the bacterial outer and inner membranes. Among them, WA7, WB11 and WD6 possessing broad-spectrum antimicrobial sensitization activity were identified as NDGA analogues with favorable properties as potential AcrB inhibitors, demonstrating moderate improvement in potency as compared to NDGA. In particular, WD6 was the most broadly active analogue improving the activity of all four classes of antibacterials tested.
The synthesis of N-phenoxyethyl-1-substituted-1,2,3,4-tetrahydroisoquinolines and their α1-adrenoceptor blocking activity
Kuo, Chen-Yuan,Wu, Ming-Jung
experimental part, p. 1271 - 1277 (2009/09/30)
A series of phenoxyisoquinolines, N-phenoxyethyl-1-(2-nitrophenyl)-1,2,3,4-THIQs 3a-3d, N-phenoxyethyl-1-benzyl-1,2,3,4-THIQ 3e, N-phenoxyethyl-1-(2-aminophenyl)-1,2,3,4-THIQs 5f-5i, N-phenoxyethyl-1-(2-phenoxyethylaminophenyl)-1,2,3,4-THIQs 5f′-5i′, have
Synthesis and?antitumor activity of?cis-dichloroplatinum(II) complexes of?1-(2-aminophenyl)-1,2,3,4-tetrahydroisoquinolines
Kuo, Chen-Yuan,Wu, Ming-Jung,Kuo, Yao-Haur
, p. 940 - 949 (2007/10/03)
Fifteen cis-dichloroplatinum complexes (5a-5o) were synthesized by treatment of 1-(2-aminophenyl)-1,2,3,4-THIQs (4a-4o) with K2PtCl4. The antitumor activity of these compounds was examined against four different human tumor cell lines. Their structure-activity relationships for antitumor activity are reported. All of these compounds exhibited activity against MCF-7 cell line and showed good activity against WiDr cell line except 5c and 5f. On the other hand, compounds 5j and 5o are more active than the other compounds against Hepa59T/VGH cell line. The electron-donating group at the 6-position of isoquinoline ring seems to decrease the antitumor activity and the chloro substituent at the C-4 position of the aniline ring shown the highest potency. The "trans influence" dominates the control of the stability of [1-(2-aminophenyl)-1,2,3,4-THIQ]dichloroplatinums(II).
Unprecedented SnCl2-mediated cyclization of nitro arenes via N-N bond formation
Sawant, Devesh,Kumar, Rishi,Maulik, Prakas R.,Kundu, Bijoy
, p. 1525 - 1528 (2007/10/03)
A mild, efficient, one-pot protocol for the cyclization of nitro-aryl substrates using SnCl2 has been described. The mechanistic course of the reaction suggests the involvement of a hydroxylamine intermediate leading to an intramolecular cyclization via N-N bond formation. The versatility of the methodology has been demonstrated by using two nitro-aryl substrates derived from dihydroisoquinolines and dihydro-β-carbolines. The intramolecular cyclization led to the formation of indazoles in high yields and purities.
A novel synthesis of 5,6-dihydroindazolo[3,2-a]isoquinolines and their relative compounds via tin(II) chloride dihydrate as reducing agent
Kuo, Chen-Yuan,Wu, Ming-Jung
, p. 965 - 974 (2007/10/03)
A series of 1-(2-nitrophenyl)-3,4-dihydroisoquinolines were reduced under very mild reaction conditions in the presence of Tin(II) chloride dihydrate (SnCl2·2H2O) to give 5,6-dihydroindazolo[3,2-a] isoquinolines 4a-h. A mechanism for
Synthesis and spectral properties of 6,7-dimethoxy-1-[(ortho; and para-R)-phenyl]-3,4-dihydroisoquinoline
Cortes Cortes,Cortes Romero,Gutierrez Ramirez
, p. 1425 - 1427 (2007/10/02)
The preparation of eleven novel 6,7-dimethoxy-1-[(ortho, and para-R)-phenyl]-3,4-dihydroisoquinolines with possible pharmacological activity is described. The structure of all products was corroborated by ir, 1H nmr, 13C-nmr, and ms.
