6926-58-5Relevant articles and documents
Developing an Anticancer Copper(II) Multitarget Pro-Drug Based on the His146 Residue in the IB Subdomain of Modified Human Serum Albumin
Wang, Jun,Gou, Yi,Zhang, Zhenlei,Yu, Ping,Qi, Jinxu,Qin, Qipin,Sun, Hongbin,Wu, Xiaoyang,Liang, Hong,Yang, Feng
, p. 2180 - 2193 (2018/05/15)
Designing a multitarget anticancer drug with improved delivery and therapeutic efficiency in vivo presents a great challenge. Thus, we proposed to design an anticancer multitarget metal pro-drug derived from thiosemicarbazone based on the His146 residue i
Isatin-β-thiosemicarbazones as potent herpes simplex virus inhibitors
Kang, Iou-Jiun,Wang, Li-Wen,Hsu, Tsu-An,Yueh, Andrew,Lee, Chung-Chi,Lee, Yen-Chun,Lee, Ching-Yin,Chao, Yu-Sheng,Shih, Shin-Ru,Chern, Jyh-Haur
scheme or table, p. 1948 - 1952 (2011/05/04)
A series of isatin-β-thiosemicarbazones have been designed and evaluated for antiviral activity against herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2) in a plaque reduction assay. Their cytotoxicity was examined using human rhabdomyosarcoma cells (RD cells). Several derivatives of isatin-β-thiosemicarbazone exhibited significant and selective antiviral activity with low cytotoxicity. It was found that the thiourea group at thiosemicarbazone and the NH functionality at isatin were essential for their antiherpetic activity. The synthesis and structure-activity relationship studies are presented.
FULLY-MODIFIED PHENYL PYRROLE AMINOGUANIDINES
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Page/Page column 74, (2009/07/17)
The invention relates to phenyl pyrrole aminoguanidines modified at the guanidine group of the general formula (I), including tautomeric and isomeric forms thereof, wherein, X is (II) and i is 0,1or 2, Y is (III) and j is 0 or 1; wherein Q is nitrogen (N)
Synthesis and antitumor activity of new thiosemicarbazones of 2-acetylimidazo[4,5-b]pyridine
Mylonas, Stavros,Mamalis, Athanasios
, p. 1273 - 1281 (2007/10/03)
A number of thiosemicarbazones of 2-acetyl-imidazo[4,5-b]pyridine were prepared in order to investigate their in vitro antineoplastic activities. Three compounds: (i) 2-acetylimidazo[4,5-b]pyridin-4-tert-butyl-3-thiosemicarbazone [(A7), NSC674098], (ii) 2-acetylimidazo[4,5-e]pyridin-4-tert-butyl-3- thiosemicarbazone [(A9), NSC674099], (iii) 2-acetylimidazo[4,5-i] pyridin-4-cyclohexyl-3-thiosemicarbozone [(A11), NSC674101] showed remarkable activity against some of the cell lines tested. The Biological Evaluation Committee of N.C.I, determined that further secondary testing should be carried out (these compounds were tested against prostate cancer).
Thiocarbamoylation of amine-containing compounds 6. Reactions of tetramethylthiuram disulfide with hydrazones of aromatic aldehydes
Boi, Luu Van,Floria, V.
, p. 344 - 347 (2007/10/03)
Thiocarbamoylation of hydrazones of aromatic aldehydes with tetramethylthiuram disulfide (TMTD) afforded diarylaldazines, 4,4-dimethylthiosemicarbazide, and 5-dimethylamino-l,3,4-thiadiazole-2-thiol. In addition, the reaction of TMTD with salicylaldehyde
2-Acetylpyridine thiosemicarbazones. II. N4,N4-disubstituted derivatives as potential antimalarial agents
Klayman,Scovill,Bartosevich,Mason
, p. 1367 - 1373 (2007/10/05)
The most effective antimalarial agents among the N4-monosubstituted 2-acetylpyridine thiosemicarbazones recently described by us have a cyclohexyl or a phenyl substituent and produce cures in Plasmodium berghei infected mice at a dose of 160 and 320 mg/kg, respectively. We report here on a related series of N4,N4-disubstituted 2-acetylpyridine thiosemicarbazones. Several members of this group bearing alkyl or cycloalkyl substituents at N4 show activity superior to the most active monosubstituted 2-acetylpyridine thiosemicarbazones. However, the greatest improvement in potency was seen when the N4-nitrogen atom was incorporated into a six- or seven-membered ring, such as the piperidine, piperazine, or azabicyclo[3.2.2]nonane systems, to give compounds with curative properties at a dose level as low as 20 mg/kg.