67449-23-4Relevant academic research and scientific papers
Quinazolin-4-one derivatives from Streptomyces isolates
Maskey, Rajendra P.,Shaaban, Mohamed,Gruen-Wollny, Iris,Laatsch, Hartmut
, p. 1131 - 1134 (2004)
From the ethyl acetate extract of the strain Streptomyces sp. isolate GW23/1540, besides 16 known products, several 1H-quinazolin-4-one derivatives were isolated. (S*R*)-2-(1-Hydroxyethyl)-2-methyl-2,3-dihydro-1H- quinazolin-4-one (4) and (R*R*)-2-(1-hydr
DIACYLGLYCEROL KINASE MODULATING COMPOUNDS
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Paragraph 1106, (2021/07/02)
The present disclosure provides diacylglycerol kinase modulating compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection. The compounds can be used alone or in combination with other agents.
Design and Discovery of an Orally Efficacious Spiroindolinone-Based Tankyrase Inhibitor for the Treatment of Colon Cancer
Shirai, Fumiyuki,Mizutani, Anna,Yashiroda, Yoko,Tsumura, Takeshi,Kano, Yuko,Muramatsu, Yukiko,Chikada, Tsubasa,Yuki, Hitomi,Niwa, Hideaki,Sato, Shin,Washizuka, Kenichi,Koda, Yasuko,Mazaki, Yui,Jang, Myung-Kyu,Yoshida, Haruka,Nagamori, Akiko,Okue, Masayuki,Watanabe, Takashi,Kitamura, Kouichi,Shitara, Eiki,Honma, Teruki,Umehara, Takashi,Shirouzu, Mikako,Fukami, Takehiro,Seimiya, Hiroyuki,Yoshida, Minoru,Koyama, Hiroo
supporting information, p. 4183 - 4204 (2020/05/20)
Tankyrases (TNKS/TNKS2) belong to the poly(ADP-ribose) polymerase family. Inhibition of their enzymatic activities attenuates the Wnt/β-catenin signaling, which plays an important role in cancer pathogenesis. We previously reported the discovery of RK-287107, a spiroindoline-based, highly selective, potent tankyrase inhibitor. Herein we describe the optimization process of RK-287107 leading to RK-582, which exhibits a markedly improved robust tumor growth inhibition in a COLO-320DM mouse xenograft model when orally administered. In addition to the dose-dependent elevation and attenuation of the levels of biomarkers AXIN2 and β-catenin, respectively, results of the TCF reporter and cell proliferation studies on COLO-320DM are discussed.
Facile and efficient synthesis of quinazoline-2,4(1H,3H)-diones through sequential hydrogenation condensation
Wang, Peng-Xu,Wang, Ya-Nan,Lin, Zi-Yun,Li, Gang,Huang, Hai-Hong
supporting information, p. 1183 - 1189 (2018/04/02)
The heterocyclizations from various methyl (2-nitrobenzoyl)carbamates to substituted quinazoline-2,4(1H,3H)-diones under hydrogenation conditions were investigated in this study. In the presence of p-toluenesulfonic acid monohydrate in methanol, various q
Synthesis of Novel Hydroxymethyl-Substituted Fused Heterocycles
Holmes, Jane L.,Almeida, Lynsie,Barlaam, Bernard,Croft, Rosemary A.,Dishington, Allan P.,Gingipalli, Laksmaiah,Hassall, Lorraine A.,Hawkins, Janet L.,Ioannidis, Stephanos,Johannes, Jeffrey W.,McGuire, Thomas M.,Moore, Jane E.,Patel, Anil,Pike, Kurt G.,Pontz, Timothy,Wu, Xiaoyun,Wang, Tao,Zhang, Hai-Jun,Zheng, Xiaolan
supporting information, p. 1226 - 1234 (2016/05/19)
Examples of hydroxymethylated analogues of heteroaryl cores such as quinazolin-4-ones, isoquinolin-1(2H)-ones, pyrido[3,4-d]pyrimidin-4(3H)-ones, chromen-4-ones and pyrrolo[2,1-f][1,2,4]triazin-4(3H)-ones are sparse or non-existent in the scientific literature. We have demonstrated that such compounds are accessible by using standard procedures from readily available raw materials.
BICYCLIC DERIVATIVE CONTAINING PYRIMIDINE RING, AND PREPARATION METHOD THEREFOR
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Paragraph 0170; 0171, (2016/04/26)
The present invention provides: a bicyclic derivative comprising a pyrimidine ring, or a pharmaceutically acceptable salt thereof; a preparation method therefor, a pharmaceutical composition comprising the same; and a use therefor. According to the present invention, the bicyclic compound derivative comprising a pyrimidine ring, or a pharmaceutically acceptable salt thereof acts as a 5-HT4 receptor agonist, and thus can be usefully applied to the prevention or treatment of dysfunction in gastrointestinal motility, for example, gastrointestinal diseases such as gastroesophageal reflux disease (GERD), constipation, irritable bowel syndrome (IBS), dyspepsia, post-operative ileus, delayed gastric emptying, gastroparesis, intestinal pseudo-obstruction, drug-induced delayed transit, diabetic gastric atony and the like.
HETEROCYCLIC COMPOUNDS AS ANTIBIOTIC POTENTIATORS
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Paragraph 0984, (2016/07/05)
The invention relates to heterocyclic compounds and their use as antibiotics and/or as antibiotic potentiators. The compounds may act as colistin potentiators and SOS inhibitors.
Pyrimidinone nicotinamide mimetics as selective tankyrase and Wnt pathway inhibitors suitable for in vivo pharmacology
Johannes, Jeffrey W.,Almeida, Lynsie,Barlaam, Bernard,Boriack-Sjodin, P. Ann,Casella, Robert,Croft, Rosemary A.,Dishington, Allan P.,Gingipalli, Lakshmaiah,Gu, Chungang,Hawkins, Janet L.,Holmes, Jane L.,Howard, Tina,Huang, Jian,Ioannidis, Stephanos,Kazmirski, Steven,Lamb, Michelle L.,McGuire, Thomas M.,Moore, Jane E.,Ogg, Derek,Patel, Anil,Pike, Kurt G.,Pontz, Timothy,Robb, Graeme R.,Su, Nancy,Wang, Haiyun,Wu, Xiaoyun,Zhang, Hai-Jun,Zhang, Yue,Zheng, Xiaolan,Wang, Tao
supporting information, p. 254 - 259 (2015/03/30)
The canonical Wnt pathway plays an important role in embryonic development, adult tissue homeostasis, and cancer. Germline mutations of several Wnt pathway components, such as Axin, APC, and ?-catenin, can lead to oncogenesis. Inhibition of the poly(ADP-r
Antileishmanial activity of a series of N2, N 4-disubstituted quinazoline-2,4-diamines
Van Horn, Kurt S.,Zhu, Xiaohua,Pandharkar, Trupti,Yang, Sihyung,Vesely, Brian,Vanaerschot, Manu,Dujardin, Jean-Claude,Rijal, Suman,Kyle, Dennis E.,Wang, Michael Zhuo,Werbovetz, Karl A.,Manetsch, Roman
, p. 5141 - 5156 (2014/07/08)
A series of N2,N4-disubstituted quinazoline-2,4- diamines has been synthesized and tested against Leishmania donovani and L. amazonensis intracellular amastigotes. A structure-activity and structure-property relationship study was conducted in part using the Topliss operational scheme to identify new lead compounds. This study led to the identification of quinazolines with EC50 values in the single digit micromolar or high nanomolar range in addition to favorable physicochemical properties. Quinazoline 23 also displayed efficacy in a murine model of visceral leishmaniasis, reducing liver parasitemia by 37% when given by the intraperitoneal route at 15 mg kg-1 day-1 for 5 consecutive days. Their antileishmanial efficacy, ease of synthesis, and favorable physicochemical properties make the N2,N 4-disubstituted quinazoline-2,4-diamine compound series a suitable platform for future development of antileishmanial agents.
A facile and convenient approach for the one-pot synthesis of 2,4(1H,3H)-quinazolinediones
Sharafi-Kolkeshvandi, Mahnaz,Nikpour, Farzad
experimental part, p. 431 - 433 (2012/06/18)
A fast and efficient method is described for the one-pot synthesis of 2,4(1H,3H)-quinazolinediones by cyclization reaction of anthranilic acid derivatives with potassium cyanate and acetic acid in PEG. Good to high yields of the products obtain in short reaction times with simple work-up.
