155 related articles for article (PubMed ID: 32763309)
1. Annulation reaction enables the identification of an exocyclic amide tricyclic chemotype as retinoic acid Receptor-Related orphan receptor gamma (RORγ/RORc) inverse agonists.
Marcoux D; Bertrand MB; Weigelt CA; Yip S; Galella M; Park H; Wu DR; Wang J; Yarde M; Cvijic ME; Li S; Hynes J; Tino JA; Zhao Q; Dhar TGM
Bioorg Med Chem Lett; 2020 Oct; 30(19):127466. PubMed ID: 32763309
[TBL] [Abstract][Full Text] [Related]
2. Tricyclic-Carbocyclic RORγt Inverse Agonists-Discovery of BMS-986313.
Yang MG; Beaudoin-Bertrand M; Xiao Z; Marcoux D; Weigelt CA; Yip S; Wu DR; Ruzanov M; Sack JS; Wang J; Yarde M; Li S; Shuster DJ; Xie JH; Sherry T; Obermeier MT; Fura A; Stefanski K; Cornelius G; Khandelwal P; Karmakar A; Basha M; Babu V; Gupta AK; Mathur A; Salter-Cid L; Denton R; Zhao Q; Dhar TGM
J Med Chem; 2021 Mar; 64(5):2714-2724. PubMed ID: 33591748
[TBL] [Abstract][Full Text] [Related]
3. Ligand-Based Design of Allosteric Retinoic Acid Receptor-Related Orphan Receptor γt (RORγt) Inverse Agonists.
Meijer FA; Doveston RG; de Vries RMJM; Vos GM; Vos AAA; Leysen S; Scheepstra M; Ottmann C; Milroy LG; Brunsveld L
J Med Chem; 2020 Jan; 63(1):241-259. PubMed ID: 31821760
[TBL] [Abstract][Full Text] [Related]
4. Identification and structure activity relationships of quinoline tertiary alcohol modulators of RORγt.
Kummer DA; Cummings MD; Abad M; Barbay J; Castro G; Wolin R; Kreutter KD; Maharoof U; Milligan C; Nishimura R; Pierce J; Schalk-Hihi C; Spurlino J; Urbanski M; Venkatesan H; Wang A; Woods C; Xue X; Edwards JP; Fourie AM; Leonard K
Bioorg Med Chem Lett; 2017 May; 27(9):2047-2057. PubMed ID: 28318945
[TBL] [Abstract][Full Text] [Related]
5. Discovery of biaryl carboxylamides as potent RORγ inverse agonists.
Chao J; Enyedy I; Van Vloten K; Marcotte D; Guertin K; Hutchings R; Powell N; Jones H; Bohnert T; Peng CC; Silvian L; Hong VS; Little K; Banerjee D; Peng L; Taveras A; Viney JL; Fontenot J
Bioorg Med Chem Lett; 2015 Aug; 25(15):2991-7. PubMed ID: 26048806
[TBL] [Abstract][Full Text] [Related]
6. Discovery of 2,6-difluorobenzyl ether series of phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfones as surprisingly potent, selective and orally bioavailable RORγt inverse agonists.
Duan JJ; Jiang B; Lu Z; Stachura S; Weigelt CA; Sack JS; Khan J; Ruzanov M; Wu DR; Yarde M; Shen DR; Zhao Q; Salter-Cid LM; Carter PH; Murali Dhar TG
Bioorg Med Chem Lett; 2020 Oct; 30(19):127441. PubMed ID: 32736080
[TBL] [Abstract][Full Text] [Related]
7. Modulators of the nuclear receptor retinoic acid receptor-related orphan receptor-γ (RORγ or RORc).
Fauber BP; Magnuson S
J Med Chem; 2014 Jul; 57(14):5871-92. PubMed ID: 24502334
[TBL] [Abstract][Full Text] [Related]
8. Tricyclic sulfones as potent, selective and efficacious RORγt inverse agonists - Exploring C6 and C8 SAR using late-stage functionalization.
Shi Q; Xiao Z; Yang MG; Marcoux D; Cherney RJ; Yip S; Li P; Wu DR; Weigelt CA; Sack J; Khan J; Ruzanov M; Wang J; Yarde M; Ellen Cvijic M; Li S; Shuster DJ; Xie J; Sherry T; Obermeier M; Fura A; Stefanski K; Cornelius G; Chacko S; Shu YZ; Khandelwal P; Hynes J; Tino JA; Salter-Cid L; Denton R; Zhao Q; Dhar TGM
Bioorg Med Chem Lett; 2020 Dec; 30(23):127521. PubMed ID: 32882417
[TBL] [Abstract][Full Text] [Related]
9. Discovery of N-(4-aryl-5-aryloxy-thiazol-2-yl)-amides as potent RORγt inverse agonists.
Wang Y; Yang T; Liu Q; Ma Y; Yang L; Zhou L; Xiang Z; Cheng Z; Lu S; Orband-Miller LA; Zhang W; Wu Q; Zhang K; Li Y; Xiang JN; Elliott JD; Leung S; Ren F; Lin X
Bioorg Med Chem; 2015 Sep; 23(17):5293-302. PubMed ID: 26277758
[TBL] [Abstract][Full Text] [Related]
10. Identification of potent, selective and orally bioavailable phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfone analogues as RORγt inverse agonists.
Lu Z; Duan JJ; Xiao H; Neels J; Wu DR; Weigelt CA; Sack JS; Khan J; Ruzanov M; An Y; Yarde M; Karmakar A; Vishwakrishnan S; Baratam V; Shankarappa H; Vanteru S; Babu V; Basha M; Kumar Gupta A; Kumaravel S; Mathur A; Zhao Q; Salter-Cid LM; Carter PH; Murali Dhar TG
Bioorg Med Chem Lett; 2019 Aug; 29(16):2265-2269. PubMed ID: 31257087
[TBL] [Abstract][Full Text] [Related]
11. Rationally Designed, Conformationally Constrained Inverse Agonists of RORγt-Identification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy.
Marcoux D; Duan JJ; Shi Q; Cherney RJ; Srivastava AS; Cornelius L; Batt DG; Liu Q; Beaudoin-Bertrand M; Weigelt CA; Khandelwal P; Vishwakrishnan S; Selvakumar K; Karmakar A; Gupta AK; Basha M; Ramlingam S; Manjunath N; Vanteru S; Karmakar S; Maddala N; Vetrichelvan M; Gupta A; Rampulla RA; Mathur A; Yip S; Li P; Wu DR; Khan J; Ruzanov M; Sack JS; Wang J; Yarde M; Cvijic ME; Li S; Shuster DJ; Borowski V; Xie JH; McIntyre KW; Obermeier MT; Fura A; Stefanski K; Cornelius G; Hynes J; Tino JA; Macor JE; Salter-Cid L; Denton R; Zhao Q; Carter PH; Dhar TGM
J Med Chem; 2019 Nov; 62(21):9931-9946. PubMed ID: 31638797
[TBL] [Abstract][Full Text] [Related]
12. Identification of N-sulfonyl-tetrahydroquinolines as RORc inverse agonists.
Fauber BP; Gobbi A; Savy P; Burton B; Deng Y; Everett C; La H; Johnson AR; Lockey P; Norman M; Wong H
Bioorg Med Chem Lett; 2015 Oct; 25(19):4109-13. PubMed ID: 26321361
[TBL] [Abstract][Full Text] [Related]
13. Optimization and biological evaluation of thiazole-bis-amide inverse agonists of RORγt.
Gege C; Albers M; Kinzel O; Kleymann G; Schlüter T; Steeneck C; Hoffmann T; Xue X; Cummings MD; Spurlino J; Milligan C; Fourie AM; Edwards JP; Leonard K; Coe K; Scott B; Pippel D; Goldberg SD
Bioorg Med Chem Lett; 2020 Jun; 30(12):127205. PubMed ID: 32336498
[TBL] [Abstract][Full Text] [Related]
14. Identification of N-phenyl-2-(N-phenylphenylsulfonamido)acetamides as new RORγ inverse agonists: Virtual screening, structure-based optimization, and biological evaluation.
Song Y; Xue X; Wu X; Wang R; Xing Y; Yan W; Zhou Y; Qian CN; Zhang Y; Xu Y
Eur J Med Chem; 2016 Jun; 116():13-26. PubMed ID: 27043267
[TBL] [Abstract][Full Text] [Related]
15. Discovery of 1-{4-[3-fluoro-4-((3s,6r)-3-methyl-1,1-dioxo-6-phenyl-[1,2]thiazinan-2-ylmethyl)-phenyl]-piperazin-1-yl}-ethanone (GNE-3500): a potent, selective, and orally bioavailable retinoic acid receptor-related orphan receptor C (RORc or RORγ) inverse agonist.
Fauber BP; René O; Deng Y; DeVoss J; Eidenschenk C; Everett C; Ganguli A; Gobbi A; Hawkins J; Johnson AR; La H; Lesch J; Lockey P; Norman M; Ouyang W; Summerhill S; Wong H
J Med Chem; 2015 Jul; 58(13):5308-22. PubMed ID: 26061388
[TBL] [Abstract][Full Text] [Related]
16. A reversed sulfonamide series of selective RORc inverse agonists.
van Niel MB; Fauber BP; Cartwright M; Gaines S; Killen JC; René O; Ward SI; de Leon Boenig G; Deng Y; Eidenschenk C; Everett C; Gancia E; Ganguli A; Gobbi A; Hawkins J; Johnson AR; Kiefer JR; La H; Lockey P; Norman M; Ouyang W; Qin A; Wakes N; Waszkowycz B; Wong H
Bioorg Med Chem Lett; 2014 Dec; 24(24):5769-5776. PubMed ID: 25453817
[TBL] [Abstract][Full Text] [Related]
17. Discovery of (3S,4S)-3-methyl-3-(4-fluorophenyl)-4-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxyprop-2-yl)phenyl)pyrrolidines as novel RORγt inverse agonists.
Jiang B; Duan JJ; Stachura S; Karmakar A; Hemagiri H; Raut DK; Gupta AK; Weigelt CA; Khan J; Sack JS; Wu DR; Yarde M; Shen DR; Galella MA; Mathur A; Zhao Q; Salter-Cid LM; Carter PH; Dhar TGM
Bioorg Med Chem Lett; 2020 Sep; 30(17):127392. PubMed ID: 32738966
[TBL] [Abstract][Full Text] [Related]
18. Design, Synthesis, and Biological Evaluation of Retinoic Acid-Related Orphan Receptor γt (RORγt) Agonist Structure-Based Functionality Switching Approach from In House RORγt Inverse Agonist to RORγt Agonist.
Yukawa T; Nara Y; Kono M; Sato A; Oda T; Takagi T; Sato T; Banno Y; Taya N; Imada T; Shiokawa Z; Negoro N; Kawamoto T; Koyama R; Uchiyama N; Skene R; Hoffman I; Chen CH; Sang B; Snell G; Katsuyama R; Yamamoto S; Shirai J
J Med Chem; 2019 Feb; 62(3):1167-1179. PubMed ID: 30652849
[TBL] [Abstract][Full Text] [Related]
19. Identification of novel quinazolinedione derivatives as RORγt inverse agonist.
Fukase Y; Sato A; Tomata Y; Ochida A; Kono M; Yonemori K; Koga K; Okui T; Yamasaki M; Fujitani Y; Nakagawa H; Koyama R; Nakayama M; Skene R; Sang BC; Hoffman I; Shirai J; Yamamoto S
Bioorg Med Chem; 2018 Feb; 26(3):721-736. PubMed ID: 29342416
[TBL] [Abstract][Full Text] [Related]
20. Structural studies unravel the active conformation of apo RORγt nuclear receptor and a common inverse agonism of two diverse classes of RORγt inhibitors.
Li X; Anderson M; Collin D; Muegge I; Wan J; Brennan D; Kugler S; Terenzio D; Kennedy C; Lin S; Labadia ME; Cook B; Hughes R; Farrow NA
J Biol Chem; 2017 Jul; 292(28):11618-11630. PubMed ID: 28546429
[TBL] [Abstract][Full Text] [Related]
[Next] [New Search]
