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Page 1
Discovery and Optimization of Novel Pyrazolopyrimidines as Potent and Orally Bioavailable Allosteric HIV-1 Integrase Inhibitors.
Li G, Meanwell NA, Krystal MR, Langley DR, Naidu BN, Sivaprakasam P, Lewis H, Kish K, Khan JA, Ng A, Trainor GL, Cianci C, Dicker IB, Walker MA, Lin Z, Protack T, Discotto L, Jenkins S, Gerritz SW, Pendri A. Li G, et al. Among authors: sivaprakasam p. J Med Chem. 2020 Mar 12;63(5):2620-2637. doi: 10.1021/acs.jmedchem.9b01681. Epub 2020 Feb 21. J Med Chem. 2020. PMID: 32081010
Discovery of new acylaminopyridines as GSK-3 inhibitors by a structure guided in-depth exploration of chemical space around a pyrrolopyridinone core.
Sivaprakasam P, Han X, Civiello RL, Jacutin-Porte S, Kish K, Pokross M, Lewis HA, Ahmed N, Szapiel N, Newitt JA, Baldwin ET, Xiao H, Krause CM, Park H, Nophsker M, Lippy JS, Burton CR, Langley DR, Macor JE, Dubowchik GM. Sivaprakasam P, et al. Bioorg Med Chem Lett. 2015 May 1;25(9):1856-63. doi: 10.1016/j.bmcl.2015.03.046. Epub 2015 Mar 24. Bioorg Med Chem Lett. 2015. PMID: 25845281
Discovery of Isonicotinamides as Highly Selective, Brain Penetrable, and Orally Active Glycogen Synthase Kinase-3 Inhibitors.
Luo G, Chen L, Burton CR, Xiao H, Sivaprakasam P, Krause CM, Cao Y, Liu N, Lippy J, Clarke WJ, Snow K, Raybon J, Arora V, Pokross M, Kish K, Lewis HA, Langley DR, Macor JE, Dubowchik GM. Luo G, et al. Among authors: sivaprakasam p. J Med Chem. 2016 Feb 11;59(3):1041-51. doi: 10.1021/acs.jmedchem.5b01550. Epub 2016 Jan 22. J Med Chem. 2016. PMID: 26751161
Uncialamycin as a novel payload for antibody drug conjugate (ADC) based targeted cancer therapy.
Chowdari NS, Pan C, Rao C, Langley DR, Sivaprakasam P, Sufi B, Derwin D, Wang Y, Kwok E, Passmore D, Rangan VS, Deshpande S, Cardarelli P, Vite G, Gangwar S. Chowdari NS, et al. Among authors: sivaprakasam p. Bioorg Med Chem Lett. 2019 Feb 1;29(3):466-470. doi: 10.1016/j.bmcl.2018.12.021. Epub 2018 Dec 11. Bioorg Med Chem Lett. 2019. PMID: 30579797
Structure-based amelioration of PXR transactivation in a novel series of macrocyclic allosteric inhibitors of HIV-1 integrase.
Sivaprakasam P, Wang Z, Meanwell NA, Khan JA, Langley DR, Johnson SR, Li G, Pendri A, Connolly TP, Gao M, Camac DM, Klakouski C, Zvyaga T, Cianci C, McAuliffe B, Ding B, Discotto L, Krystal MR, Jenkins S, Peese KM, Narasimhulu Naidu B. Sivaprakasam P, et al. Bioorg Med Chem Lett. 2020 Nov 15;30(22):127531. doi: 10.1016/j.bmcl.2020.127531. Epub 2020 Sep 2. Bioorg Med Chem Lett. 2020. PMID: 32890685
Design, Synthesis, and Structure-Activity Relationships of Novel Tetrahydroisoquinolino Benzodiazepine Dimer Antitumor Agents and Their Application in Antibody-Drug Conjugates.
Chowdari NS, Zhang Y, McDonald I, Johnson W, Langley DR, Sivaprakasam P, Mate R, Huynh T, Kotapati S, Deshpande M, Pan C, Menezes D, Wang Y, Rao C, Sarma G, Warrack BM, Rangan VS, Mei-Chen S, Cardarelli P, Deshpande S, Passmore D, Rampulla R, Mathur A, Borzilleri R, Rajpal A, Vite G, Gangwar S. Chowdari NS, et al. Among authors: sivaprakasam p. J Med Chem. 2020 Nov 25;63(22):13913-13950. doi: 10.1021/acs.jmedchem.0c01385. Epub 2020 Nov 6. J Med Chem. 2020. PMID: 33155811
DNA-Model-Based Design and Execution of Some Fused Benzodiazepine Hybrid Payloads for Antibody-Drug Conjugate Modality.
Sivaprakasam P, McDonald I, Iwuagwu C, Chowdari NS, Peese KM, Langley DR, Cheng H, Luzung MR, Schmidt MA, Zheng B, Tan Y, Cho P, Rakshit S, Lakshminarasimhan T, Guturi S, Kanagavel K, Kanusu U, Niyogi AG, Sidhar S, Vaidyanathan R, Eastgate MD, Kotapati S, Deshpande M, Pan C, Cardarelli PM, Xie C, Rao C, Holder P, Sarma G, Vite G, Gangwar S. Sivaprakasam P, et al. ACS Med Chem Lett. 2021 Feb 10;12(3):404-412. doi: 10.1021/acsmedchemlett.0c00578. eCollection 2021 Mar 11. ACS Med Chem Lett. 2021. PMID: 33738068 Free PMC article.
Design, Synthesis, and Preclinical Profiling of GSK3739936 (BMS-986180), an Allosteric Inhibitor of HIV-1 Integrase with Broad-Spectrum Activity toward 124/125 Polymorphs.
Naidu BN, Patel M, McAuliffe B, Ding B, Cianci C, Simmermacher J, Jenkins S, Parker DD, Sivaprakasam P, Khan JA, Kish K, Lewis H, Hanumegowda U, Krystal M, Meanwell NA, Kadow JF. Naidu BN, et al. Among authors: sivaprakasam p. J Med Chem. 2022 Mar 24;65(6):4949-4971. doi: 10.1021/acs.jmedchem.1c02169. Epub 2022 Mar 2. J Med Chem. 2022. PMID: 35235334
46 results