58803-74-0Relevant academic research and scientific papers
Novel quinazoline and pyrido[2,3-d]pyrimidine derivatives and their hydroselenite salts as antitumoral agents
Palop, Juan Antonio,Plano, Daniel,Moreno, Esther,Sanmartin, Carmen
, p. 187 - 206 (2014/03/21)
A series of 22 quinazolines, pyrido[2,3-d]pyrimidines and their hydroselenite salts were synthesized with the aim of evaluating in vitro their cytotoxicity against PC-3 cell line and their antioxidant properties related to DPPH (1,1-diphenyl-2-picrylhydrazylradical) activity, showing some of them better profile than the respective controls. Three of these derivatives (5d, 6d and 7f) were selected in order to gain preliminary insights to establish the mechanism of action. Caspase-3 activity and cell cycle regulation studies revealed that compound 6d provoked an increase in caspase-3 level accompanied by cell cycle perturbation in a time-dependent manner.
Sulfur and selenium derivatives of quinazoline and pyrido[2,3-d]pyrimidine: Synthesis and study of their potential cytotoxic activity in vitro
Moreno, Esther,Plano, Daniel,Lamberto, Iranzu,Font, María,Encío, Ignacio,Palop, Juan Antonio,Sanmartín, Carmen
experimental part, p. 283 - 298 (2012/02/16)
The synthesis, cytotoxic activities and selectivities of 35 derivatives related to quinazoline and pyrido[2,3-d]pyrimidine are described. The synthesized compounds were screened in vitro against four tumoral cell lines - leukemia (CCRF-CEM), colon (HT-29), lung (HTB-54) and breast (MCF-7) - and two cell lines derived from non-malignant cell lines, one mammary (184B5) and one from bronchial epithelium (BEAS-2B). MCF-7 and HTB-54 were the most sensitive cell lines with GI50 values below 10 μM for eleven and ten compounds, respectively. Two compounds (2o and 3a) were identified that evoked a marked cytotoxic effect in all cell lines tested and one compound, 7h, was potent and selective against MCF-7. A preliminary study into the mechanism of the potent derivatives 2o, 3a and 7h indicated that the cytotoxic activities of these compounds might be mediated by inducing cell death without affecting cell cycle phases.
Kilogram-scale synthesis of a highly selective α1-adrenoceptor antagonist (DL-028A)
Chou, Shan-Yen,Yin, Wei-Kung,Chung, Yuh-Shan,Chang, Lien-Shange,Liu, Chin-Wei,Chen, Shyh-Fong,Shih, Kae-Shyang
, p. 273 - 278 (2013/09/06)
This work presents an improved eight-step process, leading to kilogram quantities of high-quality DL-028A, an antihypertensive agent. The improvements include reducing the levels of toxic reagents and the removal of dangerous processes and waste gas treatment. Moreover, specification and impurity profiles were determined.
Studies on quinazolines. 6. Asymmetric synthesis of (S)-(+)- and (R)-(-)-3-[[4-(2-methoxyphenyl)piperazin-1-yl]methyl]-5-methylthio-2,3- dihydroimidazo[1,2-c]quinazolines
Gutcait, Alexander,Wang, Kuang-Chao,Liu, Hsiu-Wen,Chern, Ji-Wang
, p. 1641 - 1648 (2007/10/03)
The titled compounds have been synthesized in five steps from commercially available (R)-(+) and (S)-(-)-glycidol. The overall yield was about 29% with ee>98.5%. Copyright
