Pharmacokinetic basis for the comparative antitumour activity and toxicity of chlorambucil, phenylacetic acid mustard and ?,?-difluorochlorambucil (CB 7103) in mice

1986 ◽  
Vol 17 (1) ◽  
pp. 21-29 ◽  
Author(s):  
F. Y. F. Lee ◽  
P. Coe ◽  
P. Workman
Author(s):  
Toni Pettersson-Fernholm ◽  
Juhani Vilpo ◽  
Markus Kosonen ◽  
Kristo Hakala ◽  
Jari Hovinen

1984 ◽  
Vol 27 (1) ◽  
pp. 111-114 ◽  
Author(s):  
H. Ehrsson ◽  
I. Wallin ◽  
B. Simonsson ◽  
P. Hartvig ◽  
G. Öberg

2007 ◽  
Vol 4 (3) ◽  
pp. 406-423 ◽  
Author(s):  
Diana Florea-Wang ◽  
Inna Ijäs ◽  
Kristo Hakala ◽  
Jorma Mattinen ◽  
Juhani Vilpo ◽  
...  

2021 ◽  
Vol 22 (16) ◽  
pp. 8372
Author(s):  
Ana María Zárate ◽  
Christian Espinosa-Bustos ◽  
Simón Guerrero ◽  
Angélica Fierro ◽  
Felipe Oyarzún-Ampuero ◽  
...  

The Smoothened (SMO) receptor is the most druggable target in the Hedgehog (HH) pathway for anticancer compounds. However, SMO antagonists such as vismodegib rapidly develop drug resistance. In this study, new SMO antagonists having the versatile purine ring as a scaffold were designed, synthesised, and biologically tested to provide an insight to their mechanism of action. Compound 4s was the most active and the best inhibitor of cell growth and selectively cytotoxic to cancer cells. 4s induced cell cycle arrest, apoptosis, a reduction in colony formation and downregulation of PTCH and GLI1 expression. BODIPY-cyclopamine displacement assays confirmed 4s is a SMO antagonist. In vivo, 4s strongly inhibited tumour relapse and metastasis of melanoma cells in mice. In vitro, 4s was more efficient than vismodegib to induce apoptosis in human cancer cells and that might be attributed to its dual ability to function as a SMO antagonist and apoptosis inducer.


The Analyst ◽  
2021 ◽  
Author(s):  
Yuke Liu ◽  
Le Zhou ◽  
Jing Tan ◽  
Weiqiang Xu ◽  
Guoliang Huang ◽  
...  

Ent-11α-hydroxy-15-oxo-kaur-16-en-19-oic acid (5F), isolated and purified from Chinese herbal medicine Pteris semipinnata L., is a diterpenoid, and has been known to exert antitumour activity in several kinds of malignant cancer...


2021 ◽  
Vol 441 ◽  
pp. 213977
Author(s):  
Salvio Suárez-García ◽  
Rubén Solórzano ◽  
Ramon Alibés ◽  
Félix Busqué ◽  
Fernando Novio ◽  
...  

2021 ◽  
Vol 221 ◽  
pp. 113513
Author(s):  
Feng-Wu Liu ◽  
Shujie Ji ◽  
Yingying Gao ◽  
Yao Meng ◽  
Wenke Xu ◽  
...  
Keyword(s):  

1933 ◽  
Vol 8 (5) ◽  
pp. 447-449 ◽  
Author(s):  
Steward Basterfield ◽  
James W. Tomecko

The ionization constants of p-nitrophenylacetic and phenylmalonic acids have been determined from conductivity data. The value of K for p-nitrophenylacetic acid at 25 °C. is 1.04 × 10−4, about twice that of phenylacetic acid. The nitro group in the nucleus has not as powerful an effect on the ionization when the COOH group is in the side chain as it has when both nitro group and COOH are in the nucleus. K for p-nitrobenzoic acid is six times as great as K for benzoic acid. K for phenylmalonic acid is 2. 77 × 10−3 as compared with 1.6 × 10−3 for malonic acid.


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