cas 135631-90-2, 6-Bromo-3,4-dihydro-4,4-dimethylquinolin-2(1h)-one

Articles about 135631-90-2Total 15 be found

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Inhibitors Targeting STAT5 Signaling in Myeloid Leukemias: New Tetrahydroquinoline Derivatives with Improved Antileukemic Potential
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
Polomski, Marion,Brachet-Botineau, Marie,Juen, Ludovic,Viaud-Massuard, Marie-Claude,Gouilleux, Fabrice,Prié, Gildas
p. 1034 - 1046
(2021/01/25)

Tetrahydroquinoline units in flexible heteroarotinoids (Flex-Hets) convey anti-cancer properties in A2780 ovarian cancer cells
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
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)

CHROMAN-SUBSTITUTED, TETRAHYDROQUINOLINE-SUBSTITUTED AND THIOCHROMAN-SUBSTITUTED HETEROAROTINOIDS AS ANTI-CANCER AGENTS
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.
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Paragraph 0221; 0226; 0241; 0318

(2020/03/09)

New Inhibitor Targeting Signal Transducer and Activator of Transcription 5 (STAT5) Signaling in Myeloid Leukemias
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.
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)

Practical synthetic strategies towards lipophilic 6-iodotetrahydroquinolines and -dihydroquinolines
The synthesis of novel tetrahydroquinolines (THQ) and dihydroquinolines (DHQ) are reported using three practical, scalable synthetic approaches to access highly lipophilic analogues bearing a 6-iodo substituent, each with a different means of cyclisation. A versatile and stable quinolin-2-one intermediate was identified, which could be reduced to the corresponding THQ with borane reagents, or to the DHQ with diisobutylaluminium hydride via a novel elimination that is more favourable at higher temperatures. Coupling these strongly electron-donating scaffolds to electron-accepting moieties caused the resulting structures to exhibit strong fluorescence.
Chisholm, David R.,Zhou, Garr-Layy,Pohl, Ehmke,Valentine, Roy,Whiting, Andrew
supporting information
p. 1851 - 1862
(2016/10/05)

SUBSTITUTED BENZO[d][1,3]OXAZIN-2(4H)-ONES AND RELATED DERIVATIVES AND THEIR USES FOR MODULATING THE PROGESTERONE RECEPTOR
Compounds of formula (I), or pharmaceutically acceptable salts thereof, are provided, wherein R1-R6 and X are defined herein. Also provided are methods of preparing the compounds of formula (I), pharmaceutical compositions and kits containing a compound of formula (I), as are methods of treating endometriosis, hormone-dependent carcinomas, leiomyoma, fibroids, dysfunctional bleeding, polycystic ovary syndrome, and menopause related symptoms; methods of contraception; methods of providing hormone replacement therapy; methods of stimulating food intake; methods of synchronizing estrus; and methods of treating symptoms of premenstrual syndrome and premenstrual dysphoric disorder by administering to a mammal in need thereof a pharmaceutically effective amount of a compound of formula (I).
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Page/Page column 10-11

(2009/08/16)

Disubstituted chalcone oximes as selective agonists of RAR retinoid receptors
Compounds of the formula where the variables are as defined in the specification, are useful for preventing or treating emphysema and related pulmonary conditions of mammals and other diseases and conditions which are responsive to RARγ agonist retinoids, such as skin related diseases, including but not limited to acne and psoriasis.
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Page/Page column 20; 21

(2008/06/13)

5-[PHENYL-TETRAHYDRONAPHTHALENE-2-YL DIHYDRONAPHTHALEN-2-YL AND HETEROARYL-CYCLOPROPYL]-PENTADIENOIC ACID DERIVATIVES HAVING SERUM GLUCOSE REDUCING ACTIVITY
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.
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Page 12-13

(2010/02/10)

[3-(C5-14ALKYL-2-OXO-1,2,3,4-TETRAHYDRO-QUINOLIN-6-YL)-3-OXO-PROPENYL]-PHENYL AND [3-(C5-14ALKYL-2-OXO-1,2,3,4- TETRAHYDRO-QUINOLIN-6-YL)-3-OXO-PROPENYL]-HETEROARYL DERIVATIVES HAVING ANTI-TUMOR ACTIVITY
Compounds of the formula where the variables have the meaning defined in the specification have anti-tumor activity.
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Page column 9

(2010/02/05)

Quinazolinone and benzoxazine derivatives as progesterone receptor modulators
This invention provides compounds which are agonists and antagonists of the progesterone receptor having the general structure: wherein: R1and R2are independently selected from H, CORA, or NRBCORA, or optionally substituted alkyl, alkenyl, alknyl, cycloalklyl, aryl, or heterocyclic moieties; or R1and R2are fused to form: 3 to 8 membered spirocyclic alkyl, alkenyl or heterocyclic rings; RAis H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl groups; RBis H, C1to C3alkyl, or substituted C1to C3alkyl; R3is H, OH, NH2, CORCor optionally substituted alkyl, alkenyl, or alkynyl; RCis H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl; R4is H, halogen, CN, NO2, or optionally substituted alkyl, alkynyl, alkoxy, amino or aminoalkyl; R5is an optionally substituted benzene or five or six membered ring with 1, 2, or 3 heteroatoms selected from O, S, SO, SO2or NR6; R6is H or C1to C3alkyl; G1is O, NR7, or CR7R8; G2is CO, CS, or CR7R8; provided that when G1is O, G2is CR7R8, and G1and G2cannot both be CR7R8; R7and R8are H or an optionally substituted alkyl, aryl, or heterocyclic moiety; or pharmaceutically acceptable salt thereof, and methods using these compounds in mammals as agonists or antagonists of the progesterone receptor.
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Example 11

(2010/11/29)

Cyclic regimens using quinazolinone and benzoxazine derivatives
This invention relates to cyclic combination therapies utilizing, in combination with progestins, estrogens, or both, compounds which are progesterone receptor antagonists of the general structure: wherein: R1and R2are H, CORA, or NRBCORA, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, or heterocyclic; or R1and R2fuse to form 3 to 8 membered spirocyclic alkyl, alkenyl or heterocyclic rings; RAis H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl groups; RBis H or alkyl; R3is H, OH, NH2, CORCor alkyl, alkenyl, or alkynyl; RCis H, alkyl, aryl, alkoxy, or aminoalkyl; R4is H, halogen, CN, NO2, alkyl, alkynyl, alkoxy, amino or aminoalkyl; R5is benzene or 5- or 6-membered heterocyclic ring; R6is H or alkyl; G1is O, NR7, or CR7R8; G2is CO or CR7R8; provided that when G1is O, G2is CR7R8, and G1and G2cannot both be CR7R8; R7and R8are H or an optionally substituted alkyl, aryl, or heterocyclic moiety; or pharmaceutically acceptable salt thereof. These methods may be used for contraception or treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, prostate, or minimization of side effects or cyclic menstrual bleeding. Additional uses of the invention include stimulation of food intake.
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(2008/06/13)

Biologically active heteroarotinoids exhibiting anticancer activity and decreased toxicity
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
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)

Disubstituted acetylenes bearing heteroaromatic and heterobicyclic groups having retinoid like activity
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.
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(2008/06/13)

Acetylenes disubstituted with a phenyl or heteroaryl group and a 2-oxochromanyl, 2-oxothiochromanyl or 2-oxo-1,2,3,4-tetrahydro-quinolinyl group having retinoid-like biological activity
Compounds of the formula STR1 where R1 and R2 are hydrogen, lower alkyl of 1-6 carbons, or halogen; R3 is hydrogen, lower alkyl of 1-6 carbons, halogen, OR11, SR11, OCOR11, SCOR11, NH2, NHR11, N(R11)2, NHCOR11 or NR11 COR11 ; X is O, S or NR' where R' is hydrogen or lower alkyl of 1-6 carbons; Y is phenyl or a heteroaryl group selected from a group consisting of pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl and oxazolyl; A is (CH2)n where n is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR8, CONR9 R10, --CH2 OH, CH2 OR11, CH2 OCOR11, CHO, CH(OR12)2, CHOR13 O, --COR7, CR7 (OR 12)2, or CR7 OR13 O, where R7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R8 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R8 is phenyl or lower alkylphenyl, R9 and R10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R11 is lower alkyl, phenyl or lower alkylphenyl, R12 is lower alkyl, and R13 is divalent alkyl radical of 2-5 carbons, have retinoid-like biological activity.
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(2008/06/13)

Disubstituted acetylenes bearing heteroaromatic and heterobicyclic groups having retinoid like activity
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.
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(2008/06/13)