Design, synthesis, and X-ray structure of potent memapsin 2 (beta-secretase) inhibitors with isophthalamide derivatives as the P2-P3-ligands

Autor: Sarang S Kulkarni, Xiaoming Xu, Arun K. Ghosh, Geoffrey Bilcer, Wanpin Chang, Nagaswamy Kumaragurubaran, Gerald Koelsch, Vajira Weerasena, Robert T. Turner, Lin Hong, Jordan Tang

Publikováno v: Journal of medicinal chemistry. 50(10)

Structure-based design and synthesis of a number of potent and selective memapsin 2 inhibitors are described. These inhibitors were designed based upon the X-ray structure of memapsin 2-bound inhibitor 3 that incorporates methylsulfonyl alanine as th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ac03b68b6495efc403a8c0ece140f3a8
https://pubmed.ncbi.nlm.nih.gov/17432843

Structural Basis of Polyketide Synthase O-Methylation.

Autor: Skiba MA; Life Sciences Institute , University of Michigan , Ann Arbor , Michigan 48109 , United States.; Department of Biological Chemistry , University of Michigan , Ann Arbor , Michigan 48109 , United States., Bivins MM; Life Sciences Institute , University of Michigan , Ann Arbor , Michigan 48109 , United States., Schultz JR; Department of Medicinal Chemistry , University of Minnesota , Minneapolis , Minnesota 55455 , United States., Bernard SM; Life Sciences Institute , University of Michigan , Ann Arbor , Michigan 48109 , United States.; Chemical Biology Doctoral Program , University of Michigan , Ann Arbor , Michigan 48109 , United States., Fiers WD; Department of Medicinal Chemistry , University of Minnesota , Minneapolis , Minnesota 55455 , United States., Dan Q; Life Sciences Institute , University of Michigan , Ann Arbor , Michigan 48109 , United States., Kulkarni S; Department of Chemistry , University of Pittsburgh , Pittsburgh , Pennsylvania 15206 , United States., Wipf P; Department of Chemistry , University of Pittsburgh , Pittsburgh , Pennsylvania 15206 , United States., Gerwick WH; Center for Marine Biotechnology and Biomedicine, Scripps Institution of Oceanography , University of California San Diego , La Jolla , California 92093 , United States.; Skaggs School of Pharmacy and Pharmaceutical Sciences , University of California San Diego , La Jolla , California 92093 , United States., Sherman DH; Life Sciences Institute , University of Michigan , Ann Arbor , Michigan 48109 , United States.; Department of Medicinal Chemistry , University of Michigan , Ann Arbor , Michigan 48109 , United States.; Department of Chemistry , University of Michigan , Ann Arbor , Michigan 48109 , United States.; Department of Microbiology and Immunology , University of Michigan , Ann Arbor , Michigan 48109 , United States., Aldrich CC; Department of Medicinal Chemistry , University of Minnesota , Minneapolis , Minnesota 55455 , United States., Smith JL; Life Sciences Institute , University of Michigan , Ann Arbor , Michigan 48109 , United States.; Department of Biological Chemistry , University of Michigan , Ann Arbor , Michigan 48109 , United States.

Publikováno v: ACS chemical biology [ACS Chem Biol] 2018 Dec 21; Vol. 13 (12), pp. 3221-3228. Date of Electronic Publication: 2018 Dec 03.

Piperlongumine derived cyclic sulfonamides (sultams): Synthesis and in vitro exploration for therapeutic potential against HeLa cancer cell lines.

Autor: Lad NP; Research Centre and Post Graduate Department of Chemistry, Padmashri Vikhe Patil College of Arts, Science and Commerce, Pravaranagar, A/P Loni, Tal. Rahata, Dist. Ahmednagar 413713, India; Department of Medicinal Chemistry, Piramal Enterprises Ltd., 1-Nirlon Complex, Goregaon (East), Mumbai 400063, India., Kulkarni S; Department of Medicinal Chemistry, Piramal Enterprises Ltd., 1-Nirlon Complex, Goregaon (East), Mumbai 400063, India., Sharma R; Department of Medicinal Chemistry, Piramal Enterprises Ltd., 1-Nirlon Complex, Goregaon (East), Mumbai 400063, India., Mascarenhas M; Department of Medicinal Chemistry, Piramal Enterprises Ltd., 1-Nirlon Complex, Goregaon (East), Mumbai 400063, India., Kulkarni MR; Research Centre and Post Graduate Department of Chemistry, Padmashri Vikhe Patil College of Arts, Science and Commerce, Pravaranagar, A/P Loni, Tal. Rahata, Dist. Ahmednagar 413713, India; Department of Medicinal Chemistry, Piramal Enterprises Ltd., 1-Nirlon Complex, Goregaon (East), Mumbai 400063, India., Pandit SS; Research Centre and Post Graduate Department of Chemistry, Padmashri Vikhe Patil College of Arts, Science and Commerce, Pravaranagar, A/P Loni, Tal. Rahata, Dist. Ahmednagar 413713, India. Electronic address: akankshapandit2002@yahoo.com.

Publikováno v: European journal of medicinal chemistry [Eur J Med Chem] 2017 Jan 27; Vol. 126, pp. 870-878. Date of Electronic Publication: 2016 Dec 10.

Structure-based design, synthesis, and biological evaluation of dihydroquinazoline-derived potent β-secretase inhibitors.

Autor: Ghosh AK; Department of Chemistry, Purdue University, West Lafayette, IN 47907, United States. akghosh@purdue.edu, Pandey S, Gangarajula S, Kulkarni S, Xu X, Rao KV, Huang X, Tang J

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 Sep 01; Vol. 22 (17), pp. 5460-5. Date of Electronic Publication: 2012 Jul 20.

Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.

Autor: Tojo Y; Department of Hematology, Kumamoto University School of Medicine, 1-1-1 Honjo, Kumamoto 860-8556, Japan., Koh Y, Amano M, Aoki M, Das D, Kulkarni S, Anderson DD, Ghosh AK, Mitsuya H

Publikováno v: Antimicrobial agents and chemotherapy [Antimicrob Agents Chemother] 2010 Aug; Vol. 54 (8), pp. 3460-70. Date of Electronic Publication: 2010 May 03.