179688-03-0Relevant articles and documents
Identification of novel 4-anilinoquinazoline derivatives as potent EGFR inhibitors both under normoxia and hypoxia
Cheng, Weiyan,Yuan, Youting,Qiu, Ni,Peng, Peng,Sheng, Rong,Hu, Yongzhou
, p. 6796 - 6805 (2015/01/08)
A novel series of 4-anilinoquinazoline derivatives (19a-19t) were designed and synthesized through incorporation of the 2-nitroimidazole moiety into the 4-anilinoquinazoline scaffold of EGFR inhibitors. The most promising compound 19h displayed potent EGF
Discovery of the novel potent and selective FLT3 inhibitor 1-{5-[7-(3-morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl} -3-p-tolylurea and its anti-acute myeloid leukemia (AML) activities in vitro and in vivo
Li, Wei-Wei,Wang, Xiao-Yan,Zheng, Ren-Lin,Yan, Heng-Xiu,Cao, Zhi-Xing,Zhong, Lei,Wang, Ze-Rong,Ji, Pan,Yang, Ling-Ling,Wang, Li-Jiao,Xu, Yong,Liu, Jing-Jing,Yang, Jiao,Zhang, Chun-Hui,Ma, Shuang,Feng, Shan,Sun, Qi-Zheng,Wei, Yu-Quan,Yang, Sheng-Yong
experimental part, p. 3852 - 3866 (2012/07/14)
Structure-activity relationship (SAR) studies of 2-(quinazolin-4-ylthio) thiazole derivatives, which are for optimizing the in vitro and in vivo antiacute myeloid leukemia (AML) activity of a previously identified FLT3 inhibitor 2-(6,7-dimethoxyquinazolin-4-ylthio)thiazole (1), are described. SAR studies centering around the head (thiazole) and tails (6- and 7-positions) of the quinazoline moiety of 1 led to the discovery of a series of compounds that exhibited significantly increased potency against FLT3-driven AML MV4-11 cells. Preliminary in vivo assays were carried out on three highly active compounds, whose results showed that 1-{5-[7-(3-morpholinopropoxy)quinazolin-4-ylthio]-[1, 3,4]thiadiazol-2-yl}-3-p-tolylurea (20c) had the highest in vivo activity. Further in vitro and in vivo anti-AML studies were then performed on 20c; in an MV4-11 xenograft mouse model, a once-daily dose of 20c at 100 mg/kg for 18 days led to complete tumor regression without obvious toxicity. Western blot and immunohistochemical analysis were carried out to illustrate the mechanism of action of 20c.
Thiazole Analogues and Uses Thereof
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, (2008/06/13)
Compounds of formula (I) and salts and physiologically functional derivatives thereof, wherein R2 is attached at the 4- or 5-position of the thiazole ring and is hydrogen, alkyl, halogen, cyano, alkoxy, haloalkoxy, or alkylamino; X independently represents a divalent linkage group selected from S, O, NR4, SO, or SO2; R4 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, or heterocyclyl; R1 is attached at the 4- or 5-position of the thiazole ring and independently represents a group of formula (II): ?wherein the dotted line represents a single or double bond; * indicates the point of attachment to the thiazole ring; and n is 1, 2, or 3. Also disclosed are pharmaceutical compositions comprising the above compounds and method of treatments for cancer and other diseases.
