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Page 1
Invention of VH-937, a Potent HIV-1 Maturation Inhibitor with the Potential for Infrequent Oral Dosing in Humans.
Sit SY, Chen Y, Chen J, Venables BL, Swidorski JJ, Xu L, Sin N, Hartz RA, Lin Z, Zhang S, Li Z, Wu DR, Li P, Kempson J, Hou X, Shanmugam Y, Parker D, Jenkins S, Simmermacher J, Falk P, McAuliffe B, Cockett M, Hanumegowda U, Dicker I, Krystal M, Meanwell NA, Regueiro-Ren A. Sit SY, et al. Among authors: hanumegowda u. ACS Med Chem Lett. 2024 Oct 17;15(11):1997-2004. doi: 10.1021/acsmedchemlett.4c00419. eCollection 2024 Nov 14. ACS Med Chem Lett. 2024. PMID: 39563829
Preclinical Profile of the HIV-1 Maturation Inhibitor VH3739937.
McAuliffe B, Falk P, Chen J, Chen Y, Sit SY, Swidorski J, Hartz RA, Xu L, Venables B, Sin N, Meanwell NA, Regueiro-Ren A, Wensel D, Hanumegowda U, Krystal M. McAuliffe B, et al. Among authors: hanumegowda u. Viruses. 2024 Sep 24;16(10):1508. doi: 10.3390/v16101508. Viruses. 2024. PMID: 39459843 Free PMC article.
Potent Long-Acting Inhibitors Targeting the HIV-1 Capsid Based on a Versatile Quinazolin-4-one Scaffold.
Gillis EP, Parcella K, Bowsher M, Cook JH, Iwuagwu C, Naidu BN, Patel M, Peese K, Huang H, Valera L, Wang C, Kieltyka K, Parker DD, Simmermacher J, Arnoult E, Nolte RT, Wang L, Bender JA, Frennesson DB, Saulnier M, Wang AX, Meanwell NA, Belema M, Hanumegowda U, Jenkins S, Krystal M, Kadow JF, Cockett M, Fridell R. Gillis EP, et al. Among authors: hanumegowda u. J Med Chem. 2023 Feb 9;66(3):1941-1954. doi: 10.1021/acs.jmedchem.2c01732. Epub 2023 Jan 31. J Med Chem. 2023. PMID: 36719971
Synthesis, Structure-Activity Relationships, and In Vivo Evaluation of Novel C-17 Amine Derivatives Based on GSK3640254 as HIV-1 Maturation Inhibitors with Broad Spectrum Activity.
Hartz RA, Xu L, Sit SY, Chen J, Venables BL, Lin Z, Zhang S, Li Z, Parker D, Simmons TS, Jenkins S, Hanumegowda UM, Dicker I, Krystal M, Meanwell NA, Regueiro-Ren A. Hartz RA, et al. Among authors: hanumegowda um. J Med Chem. 2022 Dec 8;65(23):15935-15966. doi: 10.1021/acs.jmedchem.2c01618. Epub 2022 Nov 28. J Med Chem. 2022. PMID: 36441509
The Discovery of GSK3640254, a Next-Generation Inhibitor of HIV-1 Maturation.
Regueiro-Ren A, Sit SY, Chen Y, Chen J, Swidorski JJ, Liu Z, Venables BL, Sin N, Hartz RA, Protack T, Lin Z, Zhang S, Li Z, Wu DR, Li P, Kempson J, Hou X, Gupta A, Rampulla R, Mathur A, Park H, Sarjeant A, Benitex Y, Rahematpura S, Parker D, Phillips T, Haskell R, Jenkins S, Santone KS, Cockett M, Hanumegowda U, Dicker I, Meanwell NA, Krystal M. Regueiro-Ren A, et al. Among authors: hanumegowda u. J Med Chem. 2022 Sep 22;65(18):11927-11948. doi: 10.1021/acs.jmedchem.2c00879. Epub 2022 Aug 31. J Med Chem. 2022. PMID: 36044257
Discovery and Preclinical Profiling of GSK3839919, a Potent HIV-1 Allosteric Integrase Inhibitor.
Parcella K, Wang T, Eastman K, Zhang Z, Yin Z, Patel M, Tu Y, Zheng BZ, Walker MA, Saulnier MG, Frennesson D, Bowsher M, Gillis E, Peese K, Belema M, Cianci C, Dicker IB, McAuliffe B, Ding B, Falk P, Simmermacher J, Parker DD, Sivaprakasam P, Kish K, Lewis H, Hanumegowda U, Jenkins S, Kadow JF, Krystal M, Meanwell NA, Naidu BN. Parcella K, et al. Among authors: hanumegowda u. ACS Med Chem Lett. 2022 May 9;13(6):972-980. doi: 10.1021/acsmedchemlett.2c00115. eCollection 2022 Jun 9. ACS Med Chem Lett. 2022. PMID: 35707159 Free PMC article.
Scaffold modifications to the 4-(4,4-dimethylpiperidinyl) 2,6-dimethylpyridinyl class of HIV-1 allosteric integrase inhibitors.
Parcella K, Patel M, Tu Y, Eastman K, Peese K, Gillis E, Belema M, Dicker IB, McAuliffe B, Ding B, Falk P, Simmermacher J, Parker DD, Sivaprakasam P, Khan JA, Kish K, Lewis H, Hanumegowda U, Jenkins S, Kadow JF, Krystal M, Meanwell NA, Naidu BN. Parcella K, et al. Among authors: hanumegowda u. Bioorg Med Chem. 2022 Aug 1;67:116833. doi: 10.1016/j.bmc.2022.116833. Epub 2022 May 19. Bioorg Med Chem. 2022. PMID: 35605346
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: hanumegowda u. 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
Design and exploration of C-3 benzoic acid bioisosteres and alkyl replacements in the context of GSK3532795 (BMS-955176) that exhibit broad spectrum HIV-1 maturation inhibition.
Swidorski JJ, Jenkins S, Hanumegowda U, Parker DD, Beno BR, Protack T, Ng A, Gupta A, Shanmugam Y, Dicker IB, Krystal M, Meanwell NA, Regueiro-Ren A. Swidorski JJ, et al. Among authors: hanumegowda u. Bioorg Med Chem Lett. 2021 Mar 15;36:127823. doi: 10.1016/j.bmcl.2021.127823. Epub 2021 Jan 26. Bioorg Med Chem Lett. 2021. PMID: 33508465
Second Generation Inhibitors of HIV-1 Maturation.
Regueiro-Ren A, Dicker IB, Hanumegowda U, Meanwell NA. Regueiro-Ren A, et al. Among authors: hanumegowda u. ACS Med Chem Lett. 2019 Feb 8;10(3):287-294. doi: 10.1021/acsmedchemlett.8b00656. eCollection 2019 Mar 14. ACS Med Chem Lett. 2019. PMID: 30891128 Free PMC article.
36 results