70386-38-8Relevant academic research and scientific papers
Discovery of novel thieno[2,3-d]pyrimidin-4-yl hydrazone-based cyclin-dependent kinase 4 inhibitors: synthesis, biological evaluation and structure-activity relationships
Horiuchi, Takao,Takeda, Yasuyuki,Haginoya, Noriyasu,Miyazaki, Masaki,Nagata, Motoko,Kitagawa, Mayumi,Akahane, Kouichi,Uoto, Kouichi
, p. 991 - 1002 (2011/10/02)
The design, synthesis, and evaluation of novel thieno[2,3-d]pyrimidin-4-yl hydrazone analogues as cyclin-dependent kinase 4 (CDK4) inhibitors are described. In continuing our program aim to search for potent CDK4 inhibitors, the introduction of a thiazole group at the hydrazone part has led to marked enhancement of chemical stability. Furthermore, by focusing on the optimization at the C-4′ position of the thiazole ring and the C-6 position of the thieno[2,3-d]pyrimidine moiety, compound 35 has been identified with efficacy in a xenograft model of HCT116 cells. In this paper, the potency, selectivity profile, and structure-activity relationships of our synthetic compounds are discussed.
Synthesis and antiviral activity of novel 1,3,4-thiadiazine derivatives
Yang, Yajun,Feng, Ziming,Jiang, Jianshuang,Yang, Yanan,Pan, Xiandao,Zhang, Peicheng
, p. 1016 - 1019 (2011/10/08)
A series of novel 1,3,4-thiadiazine derivatives were synthesized via chemical optimization on phthiobuzone. Their anti-herpes simplex virus (HSV) activities in vitro were also tested. Several compounds exhibited more highly potent anti-HSV activity and much higher selectivity index (SI) values than those of phthiobuzone. The most potent anti-HSV compound was 4f, which showed marked inhibition against HSV-1 (IC50=77.04μg/ml) and HSV-2 (IC50=30.00μg/ml). Meanwhile it had low cytotoxicity (CC 50=1000.00μg/ml), resulting in high (SIHSV-1= 12.98, SIHSV-2=33.33, respectively). Furthermore, a computational study for prediction of absorption, distribution, metabolism, excretion (ADME) properties of compound 4f was performed by determination of topological polar surface area, absorption and Lipinski parameters.
Synthesis and antiviral activity of phthiobuzone analogues
Yang, Ya-Jun,Zhao, Jing-Hua,Pan, Xian-Dao,Zhang, Pei-Cheng
experimental part, p. 208 - 211 (2010/08/06)
A series of phthiobuzone analogs, prepared from potassium phthalimide or phthalandione, have been evaluated for their antiviral activities. Among the candidates, compounds 5j and 5k, which contain the substituted 4-halogenated phenyl ring at N-4′,4″ position, show more potent antiviral activity than phthiobuzone against herpes simplex virus 1 (IC50=8.56 and 2.85 μ/ml, respectively) and herpes simplex virus 2 (IC50=1.75 and 4.11μg/ ml, respectively). Compounds 9c and 9d with a propylene linker between the phthalimide and bisthiosemicarbazone moieties display similar antiviral potency against herpes simplex virus 1 (IC50=2.85 and 4.11 μg/ml, respectively).
Synthesis and cytotoxic activity of heterocycle-substituted phthalimide derivatives
Yang, Ya Jun,Yang, Ya Nan,Jiang, Jian Shuang,Feng, Zi Ming,Liu, Hong Yan,Pan, Xian Dao,Zhang, Pei Cheng
scheme or table, p. 902 - 904 (2011/11/30)
A series of heterocycle-substituted phthalimide derivatives were synthesized. Structurally diverse derivatives with heterocyclic rings, including furan, imidazo[1,2-a]pyridine, 1,3,4-thiadiazine, imidazo[2,1-b][1,3,4] thiadiazine, pyrazole, 1,2,4-triazolo[3,4-b][1,3,4]thiadiazine, thiazole and thiazoline, were obtained by the reactions of α-bromoketone intermediate with various nucleophiles containing oxygen, nitrogen and sulfur atom. Their cytotoxic activity was also evaluated against five human cancer cell lines in vitro.
SULFUR YLIDES. 3. SYNTHESIS OF KETO-GROUP STABILIZED AMINO-CONTAINING SULFUR YLIDES FROM AMINO ACIDS
Tolstikov, G. A.,Galin, F. Z.,Lakeev, S. N.,Khalilov, L. M.,Sultanova, V. S.
, p. 535 - 541 (2007/10/02)
An effective path of synthesis was developed of new synthetic intermediates, the optically active, keto-group stabilized amino-substituted sulfur ylides.
