16344-26-6Relevant articles and documents
Inhibition of Dihydroorotate Dehydrogenase Overcomes Differentiation Blockade in Acute Myeloid Leukemia
Sykes, David B.,Kfoury, Youmna S.,Mercier, Fran?ois E.,Wawer, Mathias J.,Law, Jason M.,Haynes, Mark K.,Lewis, Timothy A.,Schajnovitz, Amir,Jain, Esha,Lee, Dongjun,Meyer, Hanna,Pierce, Kerry A.,Tolliday, Nicola J.,Waller, Anna,Ferrara, Steven J.,Eheim, Ashley L.,Stoeckigt, Detlef,Maxcy, Katrina L.,Cobert, Julien M.,Bachand, Jacqueline,Szekely, Brian A.,Mukherjee, Siddhartha,Sklar, Larry A.,Kotz, Joanne D.,Clish, Clary B.,Sadreyev, Ruslan I.,Clemons, Paul A.,Janzer, Andreas,Schreiber, Stuart L.,Scadden, David T.
, p. 171 - 15,186 (2016)
While acute myeloid leukemia (AML) comprises many disparate genetic subtypes, one shared hallmark is the arrest of leukemic myeloblasts at an immature and self-renewing stage of development. Therapies that overcome differentiation arrest represent a power
Design, synthesis and biological evaluation of novel 4-(pyrrolo[2,3-d]pyrimidine-4-yloxy)benzamide derivatives as potential antitumor agents
Chen, Ting,Fu, Dongxue,He, Jie,Tang, Qidong,Xiong, Hehua,Yang, Feiyi,Zhang, Jianqing,Zheng, Pengwu
, (2020/12/25)
Cancer is a major cause of death worldwide. Small molecule inhibitors have become a major therapeutic treatment for cancer. In this study, a series of novel 4-(pyrrolo[2,3-d]pyrimidine-4-yloxy)benzamide derivatives were designed, synthesized and evaluated
Synthesis and antiproliferative activity of pyrrolo[2,3-b]pyridine derivatives bearing the 1,8-naphthyridin-2-one moiety
Tang, Qidong,Duan, Yongli,Wang, Linxiao,Wang, Min,Ouyang, Yiqiang,Wang, Caolin,Mei, Han,Tang, Sheng,Xiong, Yinhua,Zheng, Pengwu,Gong, Ping,Zhu, Wufu
, p. 266 - 275 (2017/12/07)
A series of pyrrolo[2,3-b]pyridine derivatives bearing the 1,8-naphthyridin-2-one moiety were synthesized, and evaluated for their antiproliferative activity against four cancer cell lines (HT-29, A549, H460, and U87MG) and six tyrosine kinases (c-Met, Flt-3, PDGFR-β VEGFR-2, EGFR, and c-Kit) inhibitory activities in vitro. Most compounds showed moderate to excellent potency, with the most promising analogue 32 showing Flt-3/c-Met IC50 value of 1.16/1.92 nM. Structure-activity relationship studies indicated that the hydrogen atom served as R1 group was benefited to the potency, and mono-electron-withdrawing groups (mono-EWGs) on the phenyl ring (such as R3 = 4-F) showed a higher preference for antiproliferative activity.
Discovery of novel 2-substituted-4-phenoxypyridine derivatives as potential antitumor agents
Duan, Yongli,Xu, Shan,Xiong, Hehua,Wang, Linxiao,Zhao, Bingbing,Wang, Ping,Wang, Caolin,Peng, Yiqing,Cai, Shifan,Luo, Rong,Zheng, Pengwu,Tang, Qidong
, p. 254 - 259 (2018/01/10)
A series of 2-substituted-4-phenoxypyridine derivatives were designed, synthesized, and evaluated for their antiproliferative activity against 4 cancer cell lines (A549, HT-29, H460, and U87MG) in vitro. Most compounds showed moderate to excellent potency. Nine tyrosine kinases (c-Met, Flt-3, ALK, VEGFR-2, VEGFR-3, PDGFR-α PDGFR-β c-Kit, and EGFR) were used to evaluate the inhibitory activities with the most promising analogue 39, which showed the Flt-3/c-Met IC50 values of 2.18/2.61 nM. Structure-activity relationship studies indicated that n-Pr served as R1 group showed a higher preference, and stronger mono-EWGs on the phenyl ring (such as R2 = 4-F) was benefited to the potency.
Synthesis and antiproliferative activity of 6,7-disubstituted-4-phenoxyquinoline derivatives bearing the 1,8-naphthyridin-2-one moiety
Tang, Qidong,Duan, Yongli,Xiong, Hehua,Chen, Ting,Xiao, Zhen,Wang, Linxiao,Xiao, Yueyue,Huang, Shunmin,Xiong, Yinhua,Zhu, Wufu,Gong, Ping,Zheng, Pengwu
, p. 201 - 213 (2018/09/18)
A series of 6,7-disubstituted-4-phenoxyquinoline derivatives bearing the 1,8-naphthyridin-2-one moiety were designed, synthesized and evaluated for their biological activities. The target compounds exhibited moderate to high antiproliferative activity against three cancer cell lines (A549, HepG2 and MCF-7) and several compounds (25, 27, 33, 37, 41, 43, 49 and 53) were evaluated for the activity against c-Met kinase. The most promising compound 33 (IC50 c-Met = 2.36 nM) showed excellent activity against A549, HepG2 and MCF-7 cell lines with IC50 values of 0.23 μM, 0.42 μM and 0.21 μM, respectively, which was 1.5–2.1 times of the positive control. Furthermore, compound 33 was evaluated for the activity against Flt3, PDGFR-α PDGFR-β c-Kit, Flt4, ALK and EGFR kinase. Structure activity relationship studies indicated that mono-EWGs (such as R2 = F) at 4-position of moiety C was a key factor in improving the antitumor activity. In addition, further research on compound 33 was mainly including concentration dependence, apoptosis (acridine orange staining), apoptosis result analyzing and molecular docking.
COMPOUNDS AND METHODS USEFUL FOR TREATING OR PREVENTING HEMATOLOGICAL CANCERS
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Page/Page column 52, (2017/03/28)
The present invention includes methods of treating patients with acute myeloid leukemia across a range of genetic subtypes with DHODH inhibitors, such as 6-fluoro-2-(2'-fluoro-[1,1'- biphenyl]-4-yl)-3-methylquinoline-4-carboxylic acid).
Development of ML390: A Human DHODH Inhibitor That Induces Differentiation in Acute Myeloid Leukemia
Lewis, Timothy A.,Sykes, David B.,Law, Jason M.,Mu?oz, Benito,Rustiguel, Joane K.,Nonato, Maria Cristina,Scadden, David T.,Schreiber, Stuart L.
supporting information, p. 1112 - 1117 (2016/12/16)
Homeobox transcription factor A9 (HoxA9) is overexpressed in 70% of patients diagnosed with acute myeloid leukemia (AML), whereas only a small subset of AML patients respond to current differentiation therapies. A cell line overexpressing HoxA9 was derive
Synthesis and mechanistic aspects of 2-anilinonicotinyl-pyrazolo[1,5-a]pyrimidine conjugates that regulate cell proliferation in MCF-7 cells via estrogen signaling
Kamal, Ahmed,Faazil, Shaikh,Hussaini, S.M. Ali,Ramaiah, M. Janaki,Balakrishna,Patel, Nibedita,Pushpavalli,Pal-Bhadra, Manika
, p. 2077 - 2083 (2016/04/05)
A series of anilinonicotinyl linked pyrazolo[1,5-a]pyrimidine conjugates (6a-x) were synthesized and evaluated for their antiproliferative activity. Some of these conjugates exhibited promising cytotoxic effects in the MCF-7 cell line and among these 6a a
2-ANILINO NICOTINYL LINKED 2-AMINO BENZOTHIAZOLE CONJUGATES AND PROCESS FOR THE PREPARATION THEREOF
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, (2014/01/07)
The present invention provides compounds of general formula A useful as potential anticancer agents against human cancer cell lines and apoptosis inducers. The present invention further provides a process for the preparation of 2-anilino nicotinyl linked 2-amino benzothiazole conjugates of general formula (A), wherein R1═H or CI; R2═H, OCH3 or F; R3═H, OCH3, F or CI; R4═H, OCH3 or F and X═OCH3, F or N02.
Synthesis of 2-(arylamino)nicotinic acids in high-temperature water
Li, Zhenghua,Xiao, Shangyou,Liang, Ronghui,Xia, Zhining
, p. 1691 - 1697 (2012/10/29)
In hydrothermal reactions at 150-180 °C, 2-(arylamino)nicotinic acids were synthesized by amination of 2-chloronicotinic acid with aromatic amine derivatives, with potassium carbonate as base. The procedure is efficient, environmentally friendly, and practical, with moderate to excellent yields (up to 98%). Springer Science+Business Media B.V. 2012.