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Page 1
Discovery, Optimization, and Biological Evaluation of Arylpyridones as Cbl-b Inhibitors.
Mfuh AM, Boerth JA, Bommakanti G, Chan C, Chinn AJ, Code E, Fricke PJ, Giblin KA, Gohlke A, Hansel C, Hariparsad N, Hughes SJ, Jin M, Kantae V, Kavanagh SL, Lamb ML, Lane J, Moore R, Puri T, Quinn TR, Reddy I, Robb GR, Robbins KJ, Gancedo Rodrigo M, Schimpl M, Singh B, Singh M, Tang H, Thomson C, Walsh JJ, Ware J, Watson IDG, Ye MW, Wrigley GL, Zhang AX, Zhang Y, Grimster NP. Mfuh AM, et al. Among authors: kavanagh sl. J Med Chem. 2024 Jan 25;67(2):1500-1512. doi: 10.1021/acs.jmedchem.3c02083. Epub 2024 Jan 16. J Med Chem. 2024. PMID: 38227216
Discovery of a Novel Benzodiazepine Series of Cbl-b Inhibitors for the Enhancement of Antitumor Immunity.
Boerth JA, Chinn AJ, Schimpl M, Bommakanti G, Chan C, Code EL, Giblin KA, Gohlke A, Hansel CS, Jin M, Kavanagh SL, Lamb ML, Lane JS, Larner CJB, Mfuh AM, Moore RK, Puri T, Quinn TR, Ye M, Robbins KJ, Gancedo-Rodrigo M, Tang H, Walsh J, Ware J, Wrigley GL, Reddy IK, Zhang Y, Grimster NP. Boerth JA, et al. Among authors: kavanagh sl. ACS Med Chem Lett. 2023 Nov 17;14(12):1848-1856. doi: 10.1021/acsmedchemlett.3c00439. eCollection 2023 Dec 14. ACS Med Chem Lett. 2023. PMID: 38116444 Free PMC article.
Discovery of a Potent and Orally Bioavailable Zwitterionic Series of Selective Estrogen Receptor Degrader-Antagonists.
Scott JS, Stead D, Barlaam B, Breed J, Carbajo RJ, Chiarparin E, Cureton N, Davey PRJ, Fisher DI, Gangl ET, Grebe T, Greenwood RD, Hande S, Hatoum-Mokdad H, Hughes SJ, Hunt TA, Johnson T, Kavanagh SL, Klinowska TCM, Larner CJB, Lawson M, Lister AS, Longmire D, Marden S, McGuire TM, McMillan C, McMurray L, Morrow CJ, Nissink JWM, Moss TA, O'Donovan DH, Polanski R, Stokes S, Thakur K, Trueman D, Truman C, Tucker MJ, Wang H, Whalley N, Wu D, Wu Y, Yang B, Yang W. Scott JS, et al. Among authors: kavanagh sl. J Med Chem. 2023 Feb 23;66(4):2918-2945. doi: 10.1021/acs.jmedchem.2c01964. Epub 2023 Feb 1. J Med Chem. 2023. PMID: 36727211
Discovery of Imidazo[1,2-a]pyridine Ethers and Squaramides as Selective and Potent Inhibitors of Mycobacterial Adenosine Triphosphate (ATP) Synthesis.
Tantry SJ, Markad SD, Shinde V, Bhat J, Balakrishnan G, Gupta AK, Ambady A, Raichurkar A, Kedari C, Sharma S, Mudugal NV, Narayan A, Naveen Kumar CN, Nanduri R, Bharath S, Reddy J, Panduga V, Prabhakar KR, Kandaswamy K, Saralaya R, Kaur P, Dinesh N, Guptha S, Rich K, Murray D, Plant H, Preston M, Ashton H, Plant D, Walsh J, Alcock P, Naylor K, Collier M, Whiteaker J, McLaughlin RE, Mallya M, Panda M, Rudrapatna S, Ramachandran V, Shandil R, Sambandamurthy VK, Mdluli K, Cooper CB, Rubin H, Yano T, Iyer P, Narayanan S, Kavanagh S, Mukherjee K, Balasubramanian V, Hosagrahara VP, Solapure S, Ravishankar S, Hameed P S. Tantry SJ, et al. J Med Chem. 2017 Feb 23;60(4):1379-1399. doi: 10.1021/acs.jmedchem.6b01358. Epub 2017 Feb 3. J Med Chem. 2017. PMID: 28075132
Discovery of AZD9833, a Potent and Orally Bioavailable Selective Estrogen Receptor Degrader and Antagonist.
Scott JS, Moss TA, Balazs A, Barlaam B, Breed J, Carbajo RJ, Chiarparin E, Davey PRJ, Delpuech O, Fawell S, Fisher DI, Gagrica S, Gangl ET, Grebe T, Greenwood RD, Hande S, Hatoum-Mokdad H, Herlihy K, Hughes S, Hunt TA, Huynh H, Janbon SLM, Johnson T, Kavanagh S, Klinowska T, Lawson M, Lister AS, Marden S, McGinnity DF, Morrow CJ, Nissink JWM, O'Donovan DH, Peng B, Polanski R, Stead DS, Stokes S, Thakur K, Throner SR, Tucker MJ, Varnes J, Wang H, Wilson DM, Wu D, Wu Y, Yang B, Yang W. Scott JS, et al. J Med Chem. 2020 Dec 10;63(23):14530-14559. doi: 10.1021/acs.jmedchem.0c01163. Epub 2020 Sep 29. J Med Chem. 2020. PMID: 32910656
Discovery of Clinical Candidate AZD0095, a Selective Inhibitor of Monocarboxylate Transporter 4 (MCT4) for Oncology.
Goldberg FW, Kettle JG, Lamont GM, Buttar D, Ting AKT, McGuire TM, Cook CR, Beattie D, Morentin Gutierrez P, Kavanagh SL, Komen JC, Kawatkar A, Clark R, Hopcroft L, Hughes G, Critchlow SE. Goldberg FW, et al. Among authors: kavanagh sl. J Med Chem. 2023 Jan 12;66(1):384-397. doi: 10.1021/acs.jmedchem.2c01342. Epub 2022 Dec 16. J Med Chem. 2023. PMID: 36525250
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
Naik M, Humnabadkar V, Tantry SJ, Panda M, Narayan A, Guptha S, Panduga V, Manjrekar P, Jena LK, Koushik K, Shanbhag G, Jatheendranath S, Manjunatha MR, Gorai G, Bathula C, Rudrapatna S, Achar V, Sharma S, Ambady A, Hegde N, Mahadevaswamy J, Kaur P, Sambandamurthy VK, Awasthy D, Narayan C, Ravishankar S, Madhavapeddi P, Reddy J, Prabhakar K, Saralaya R, Chatterji M, Whiteaker J, McLaughlin B, Chiarelli LR, Riccardi G, Pasca MR, Binda C, Neres J, Dhar N, Signorino-Gelo F, McKinney JD, Ramachandran V, Shandil R, Tommasi R, Iyer PS, Narayanan S, Hosagrahara V, Kavanagh S, Dinesh N, Ghorpade SR. Naik M, et al. J Med Chem. 2014 Jun 26;57(12):5419-34. doi: 10.1021/jm5005978. Epub 2014 Jun 11. J Med Chem. 2014. PMID: 24871036
Development of Pyrazolopyrimidine Anti-Wolbachia Agents for the Treatment of Filariasis.
McGillan P, Berry NG, Nixon GL, Leung SC, Webborn PJH, Wenlock MC, Kavanagh S, Cassidy A, Clare RH, Cook DA, Johnston KL, Ford L, Ward SA, Taylor MJ, Hong WD, O'Neill PM. McGillan P, et al. ACS Med Chem Lett. 2021 Aug 20;12(9):1421-1426. doi: 10.1021/acsmedchemlett.1c00216. eCollection 2021 Sep 9. ACS Med Chem Lett. 2021. PMID: 34527179 Free PMC article.
Aminoazabenzimidazoles, a novel class of orally active antimalarial agents.
Hameed P S, Chinnapattu M, Shanbag G, Manjrekar P, Koushik K, Raichurkar A, Patil V, Jatheendranath S, Rudrapatna SS, Barde SP, Rautela N, Awasthy D, Morayya S, Narayan C, Kavanagh S, Saralaya R, Bharath S, Viswanath P, Mukherjee K, Bandodkar B, Srivastava A, Panduga V, Reddy J, Prabhakar KR, Sinha A, Jiménez-Díaz MB, Martínez MS, Angulo-Barturen I, Ferrer S, Sanz LM, Gamo FJ, Duffy S, Avery VM, Magistrado PA, Lukens AK, Wirth DF, Waterson D, Balasubramanian V, Iyer PS, Narayanan S, Hosagrahara V, Sambandamurthy VK, Ramachandran S. Hameed P S, et al. J Med Chem. 2014 Jul 10;57(13):5702-13. doi: 10.1021/jm500535j. Epub 2014 Jun 24. J Med Chem. 2014. PMID: 24914738
12 results