385784-71-4Relevant academic research and scientific papers
4-heterocycle substituted quinazoline derivative and preparation method and application thereof
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, (2020/02/19)
The invention discloses a 4-heterocycle substituted quinazoline derivative and a preparation method and application thereof. The compound has a structure expressed by a general formula (I): (please see the specification for the formula), in the formula, R1 and R2 are independently selected from hydrogen, a saturated or unsaturated five-membered heterocycle, or a saturated or unsaturated six-membered heterocycle, and n is an integer from 1 to 6; X is NH, O or S; and a heterocycle A is independently selected from pyridine or substituted pyridine, pyrimidine or substituted pyrimidine, pyrazol orsubstituted pyrazol, pyrazine or substituted pyrazine, thiazole or substituted thiazole, or benzothiazole or substituted benzothiazole. The compound or pharmaceutically formable salts thereof have aninhibitory effect on proliferation of tumor cells and can be used for preparing drugs for treatment of glioma, non-small cell lung cancer, breast cancer, colon cancer, stomach cancer, liver cancer andcervical cancer diseases.
One-pot conversion of 2-nitrobenzonitriles to quinazolin-4(3H)-ones and synthesis of gefitinib and erlotinib hydrochloride
Chandregowda, Venkateshappa,Venkateswara Rao, Gudapati,Chandrasekara Reddy, Goukanapalli
, p. 39 - 48 (2008/02/02)
A simple and efficient one-pot conversion of 2-nitrobenzonitriles to quinazolin-4(3H)-ones involving reduction, formylation, hydrolysis and cyclization is reported. These quinazolinones have been used for making in economical way the anticancer drug molecules gefitinib (Iressa) and erlotinib HCl (Tarceva).
Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors
Jung, Frédéric H.,Pasquet, Georges,Lambert-Van Der Brempt, Christine,Lohmann, Jean-Jacques M.,Warin, Nicolas,Renaud, Fabrice,Germain, Hervé,De Savi, Chris,Roberts, Nicola,Johnson, Trevor,Dousson, Cyril,Hill, George B.,Mortlock, Andrew A.,Heron, Nicola,Wilkinson, Robert W.,Wedge, Stephen R.,Heaton, Simon P.,Odedra, Rajesh,Keen, Nicholas J.,Green, Stephen,Brown, Elaine,Thompson, Katherine,Brightwell, Stephen
, p. 955 - 970 (2007/10/03)
The synthesis of a novel series of quinazolines substituted at C4 by five-membered ring aminoheterocycles is reported. Their in vitro structure-activity relationships versus Aurora A and B serine-threonine kinases is discussed. Our results demonstrate tha
