135631-91-3Relevant academic research and scientific papers
Inhibitors Targeting STAT5 Signaling in Myeloid Leukemias: New Tetrahydroquinoline Derivatives with Improved Antileukemic Potential
Polomski, Marion,Brachet-Botineau, Marie,Juen, Ludovic,Viaud-Massuard, Marie-Claude,Gouilleux, Fabrice,Prié, Gildas
, p. 1034 - 1046 (2021/01/25)
Signal transducers and activators of transcription 5A and 5B (STAT5A and STAT5B) are two closely related STAT family members that are crucial downstream effectors of tyrosine kinase oncoproteins such as FLT3-ITD in acute myeloid leukemia (AML) and BCR-ABL
Tetrahydroquinoline units in flexible heteroarotinoids (Flex-Hets) convey anti-cancer properties in A2780 ovarian cancer cells
Gnanasekaran, Krishna Kumar,Pouland, Tim,Bunce, Richard A.,Darrell Berlin,Abuskhuna, Suaad,Bhandari, Dipendra,Mashayekhi, Maryam,Zhou, Donghua H.,Benbrook, Doris M.
, (2019/12/24)
SHetA2 (NSC 721689), our lead Flex-Het anti-cancer agent, consists of a thiochroman (Ring A) and a 4-nitrophenyl (Ring B) linked by a thiourea bridge. In this work, several series of new analogs having a tetrahydroquinoline (THQ, Ring A) unit connected by
CHROMAN-SUBSTITUTED, TETRAHYDROQUINOLINE-SUBSTITUTED AND THIOCHROMAN-SUBSTITUTED HETEROAROTINOIDS AS ANTI-CANCER AGENTS
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Paragraph 0221; 0226; 0241; 0319, (2020/03/09)
Chemical compounds that inhibit cancer cell growth are provided. The compounds are heteroarotinoids and derivatives thereof with oxygen, nitrogen or sulfur in chroman systems, tetrahydroquinoline systems, and tetrahydrothiochroman systems.
New Inhibitor Targeting Signal Transducer and Activator of Transcription 5 (STAT5) Signaling in Myeloid Leukemias
Juen, Ludovic,Brachet-Botineau, Marie,Parmenon, Cécile,Bourgeais, Jér?me,Hérault, Olivier,Gouilleux, Fabrice,Viaud-Massuard, Marie-Claude,Prié, Gildas
, p. 6119 - 6136 (2017/08/02)
Signal transducers and activators of transcription 5 (STAT5s) are crucial effectors of tyrosine kinase oncogenes in myeloid leukemias. Inhibition of STAT5 would contribute to reducing the survival of leukemic cells and also tackling their chemoresistance. In a first screening experiment, we identified hit 13 as able to inhibit STAT5 phosphorylation and leukemic cell growth. The synthesis of 18 analogues of 13 allowed us to identify one compound, 17f, as having the most potent antileukemic effect. 17f inhibited the growth of acute and chronic myeloid leukemia cells and the phosphorylation and transcriptional activity of STAT5. Importantly, 17f had minimal effects on bone marrow stromal cells that play vital functions in the microenvironment of hematopoietic and leukemic cells. We also demonstrated that 17f inhibits STAT5 but not STAT3, AKT, or Erk1/2 phosphorylation. These results suggest that 17f might be a new lead molecule targeting STAT5 signaling in myeloid leukemias.
5-[PHENYL-TETRAHYDRONAPHTHALENE-2-YL DIHYDRONAPHTHALEN-2-YL AND HETEROARYL-CYCLOPROPYL]-PENTADIENOIC ACID DERIVATIVES HAVING SERUM GLUCOSE REDUCING ACTIVITY
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Page 13, (2010/02/10)
Compounds of the formula where the variables have the meaning defined in the specification are capable of reducing serum glucose levels in diabetic mammals without the undesirable side effects of reducing serum thyroxine levels and transiently increasing triglyceride levels.
Synthesis and biological activity of 1,2,3,4-tetrahydroquinoline and 3,4-(1H)-dihydroquinolin-2-one analogs of retinoic acid
Beard, Richard L.,Teng, Min,Colon, Diana F.,Duong, Tien T.,Thacher, Scott M.,Arefieg, Taghreed,Chandraratna, Roshantha A.S.
, p. 2373 - 2378 (2007/10/03)
Retinoids are natural and synthetic analogs of the hormone retinoic acid. Retinoids are currently being investigated clinically as drugs in several areas, including dermatology and oncology. We report the synthesis and biological activity of a new series of potent, RAR-specific retinoids substituted with a 1,2,3,4-tetrahydroquinoline or a 3,4-1H)-dihydroquinolin-2-one group.
Biologically active heteroarotinoids exhibiting anticancer activity and decreased toxicity
Benbrook, Doris M.,Madler, Matora M.,Spruce, Lyle W.,Birckbichler, Paul J.,Nelson, Eldon C.,Subramanian, Shankar,Mahika Weerasekare,Gale, Jonathan B.,Patterson Jr., Manford K.,Wang, Binghe,Wang, Wei,Lu, Shennan,Rowland, Tami C.,DiSivestro, Paul,Lindamood III, Charles,Hill, Donald L.,Berlin, K. Darrell
, p. 3567 - 3583 (2007/10/03)
A series of retinoids, containing heteroatoms in a cyclic ring and called heteroarotinoids, were synthesized, and their biological activity was evaluated using tissue culture lines that have measurable responses to trans- retinoic acid (t-RA). Transglutam
Disubstituted acetylenes bearing heteroaromatic and heterobicyclic groups having retinoid like activity
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, (2008/06/13)
Retinoid-like activity is exhibited by compounds of the formula STR1 where X is S, O, or NR' where R' is hydrogen or lower alkyl; R is hydrogen or lower alkyl; A is pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl or pyrazinyl; n is 0-4; and B is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH2 OH or an ether or ester derivative, or --CHO or an acetal derivative, or --COR1 or a ketal derivative where R1 is --(CH2)m CH3 where m is 0-4, or a pharmaceutically acceptable salt thereof.
Disubstituted acetylenes bearing heteroaromatic and heterobicyclic groups having retinoid like activity
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, (2008/06/13)
Retinoid-like activity is exhibited by compounds of the formula STR1 where X is S, O, or NR' where R' is hydrogen or lower alkyl; R is hydrogen or lower alkyl; A is pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl or pyrazinyl; n is 0-2; and B is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH2 OH or an ether or ester derivative, or --CHO or an acetal derivative, or --COR1 or a ketal derivative where R1 is --(CH2)m CH3 where m is 0-4, or a pharmaceutically acceptable salt thereof.
