Empowering Voices: Inspiring Women in Medicinal Chemistry.

Autor: Blanco MJ, Bronson JJ, DiMauro EF, Dzierba C, Eggen M, Garner AL, Georg G, Giarolla J, Goodwin NC, Grenier-Davies MC, Haskell-Luevano C, Holzgrabe U, Huang R, Lagiakos HR, Leftheris K, Martin Y, Matos MJ, May-Dracka TL, Müller CE, Newman AH, Parmee E, Petter JC, Tamayo NA, Wexler RR, Bolognesi ML, Ripka A, Young W

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2024 Mar 28; Vol. 67 (6), pp. 4251-4258. Date of Electronic Publication: 2024 Mar 08.

Discovery of a highly potent, selective, orally bioavailable inhibitor of KAT6A/B histone acetyltransferases with efficacy against KAT6A-high ER+ breast cancer.

Autor: Sharma S; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA. Electronic address: shikhar.sharma@pfizer.com., Chung CY; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Uryu S; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Petrovic J; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Cao J; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Rickard A; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Nady N; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Greasley S; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Johnson E; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Brodsky O; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Khan S; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Wang H; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Wang Z; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Zhang Y; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Tsaparikos K; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Chen L; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Mazurek A; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Lapek J; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Kung PP; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Sutton S; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Richardson PF; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Greenwald EC; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Yamazaki S; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Jones R; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Maegley KA; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Bingham P; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Lam H; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Stupple AE; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Medicinal Chemistry and Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia; CANThera Discovery, Melbourne, VIC 3000, Australia., Kamal A; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia., Chueh A; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia., Cuzzupe A; SYNthesis Med Chem (Australia) Pty Ltd, Bio21 Institute, 30 Flemington Road, Parkville, VIC 3052, Australia., Morrow BJ; Medicinal Chemistry and Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia., Ren B; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Commonwealth Scientific and Industrial Research Organisation (CSIRO), Parkville, VIC 3052, Australia., Carrasco-Pozo C; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Discovery Biology, Centre for Cellular Phenomics, Griffith University, Brisbane QLD 4111, Australia., Tan CW; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3052, Australia., Bhuva DD; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3052, Australia., Allan E; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia., Surgenor E; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia., Vaillant F; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3052, Australia., Pehlivanoglu H; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia., Falk H; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3052, Australia; Commonwealth Scientific and Industrial Research Organisation (CSIRO), Parkville, VIC 3052, Australia., Whittle JR; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3052, Australia., Newman J; Commonwealth Scientific and Industrial Research Organisation (CSIRO), Parkville, VIC 3052, Australia., Cursons J; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia., Doherty JP; Peter MacCallum Cancer Centre, Melbourne VIC 3000, Australia; Sir Peter MacCallum Department of Oncology, The University of Melbourne, Parkville, VIC 3052, Australia., White KL; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Medicinal Chemistry and Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia., MacPherson L; Peter MacCallum Cancer Centre, Melbourne VIC 3000, Australia; Sir Peter MacCallum Department of Oncology, The University of Melbourne, Parkville, VIC 3052, Australia., Devlin M; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Peter MacCallum Cancer Centre, Melbourne VIC 3000, Australia; Sir Peter MacCallum Department of Oncology, The University of Melbourne, Parkville, VIC 3052, Australia., Dennis ML; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Commonwealth Scientific and Industrial Research Organisation (CSIRO), Parkville, VIC 3052, Australia., Hattarki MK; Commonwealth Scientific and Industrial Research Organisation (CSIRO), Parkville, VIC 3052, Australia., De Silva M; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia., Camerino MA; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Medicinal Chemistry and Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia., Butler MS; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Peter MacCallum Cancer Centre, Melbourne VIC 3000, Australia; Sir Peter MacCallum Department of Oncology, The University of Melbourne, Parkville, VIC 3052, Australia., Dolezal O; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Commonwealth Scientific and Industrial Research Organisation (CSIRO), Parkville, VIC 3052, Australia., Pilling P; Commonwealth Scientific and Industrial Research Organisation (CSIRO), Parkville, VIC 3052, Australia., Foitzik R; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Medicinal Chemistry and Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia; OncologyOne Pty Ltd, Melbourne, VIC 3000, Australia., Stupple PA; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Medicinal Chemistry and Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia; CANThera Discovery, Melbourne, VIC 3000, Australia., Lagiakos HR; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Medicinal Chemistry and Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia., Walker SR; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Medicinal Chemistry and Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia; Commonwealth Scientific and Industrial Research Organisation (CSIRO), Parkville, VIC 3052, Australia., Hediyeh-Zadeh S; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3052, Australia., Nuttall S; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Commonwealth Scientific and Industrial Research Organisation (CSIRO), Parkville, VIC 3052, Australia., Spall SK; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia., Charman SA; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Medicinal Chemistry and Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia., Connor T; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Peter MacCallum Cancer Centre, Melbourne VIC 3000, Australia; Sir Peter MacCallum Department of Oncology, The University of Melbourne, Parkville, VIC 3052, Australia., Peat TS; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Commonwealth Scientific and Industrial Research Organisation (CSIRO), Parkville, VIC 3052, Australia., Avery VM; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Discovery Biology, Centre for Cellular Phenomics, Griffith University, Brisbane QLD 4111, Australia., Bozikis YE; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Medicinal Chemistry and Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia., Yang Y; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3052, Australia., Zhang M; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia., Monahan BJ; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3052, Australia; CANThera Discovery, Melbourne, VIC 3000, Australia., Voss AK; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3052, Australia., Thomas T; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3052, Australia., Street IP; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3052, Australia; OncologyOne Pty Ltd, Melbourne, VIC 3000, Australia; Children's Cancer Institute, Randwick, NSW 2031, Australia; University of New South Wales, Randwick, NSW 2021, Australia., Dawson SJ; Peter MacCallum Cancer Centre, Melbourne VIC 3000, Australia; Sir Peter MacCallum Department of Oncology, The University of Melbourne, Parkville, VIC 3052, Australia., Dawson MA; Peter MacCallum Cancer Centre, Melbourne VIC 3000, Australia; Sir Peter MacCallum Department of Oncology, The University of Melbourne, Parkville, VIC 3052, Australia., Lindeman GJ; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medicine, Royal Melbourne Hospital, The University of Melbourne, Parkville, VIC 3010, Australia; Parkville Familial Cancer Centre and Department of Medical Oncology, The Royal Melbourne Hospital and Peter MacCallum Cancer Centre, Parkville, VIC 3050, Australia., Davis MJ; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3052, Australia; Department of Clinical Pathology, Faculty of Medicine, Dentistry and Health Sciences, University of Melbourne, Parkville, VIC 3010, Australia., Visvader JE; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3052, Australia., Paul TA; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA. Electronic address: thomas.a.paul@pfizer.com.

Publikováno v: Cell chemical biology [Cell Chem Biol] 2023 Oct 19; Vol. 30 (10), pp. 1191-1210.e20. Date of Electronic Publication: 2023 Aug 08.

In Vitro and In Vivo Inhibition of the Mycobacterium tuberculosis Phosphopantetheinyl Transferase PptT by Amidinoureas.

Autor: Ottavi S; Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States., Scarry SM; Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States., Mosior J; Departments of Biochemistry and Biophysics, Texas Agricultural and Mechanical University, College Station, Texas 77843, United States., Ling Y; Department of Microbiology & Immunology, Weill Cornell Medicine, New York, New York 10065, United States., Roberts J; Department of Microbiology & Immunology, Weill Cornell Medicine, New York, New York 10065, United States., Singh A; Department of Microbiology & Immunology, Weill Cornell Medicine, New York, New York 10065, United States., Zhang D; Department of Microbiology & Immunology, Weill Cornell Medicine, New York, New York 10065, United States., Goullieux L; Evotec ID (Lyon), SAS 40 Avenue Tony Garnier, Lyon 69001, France., Roubert C; Evotec ID (Lyon), SAS 40 Avenue Tony Garnier, Lyon 69001, France., Bacqué E; Evotec ID (Lyon), SAS 40 Avenue Tony Garnier, Lyon 69001, France., Lagiakos HR; Schrödinger, Inc., 120 W. 45 Street, New York, New York 10036, United States., Vendome J; Schrödinger, Inc., 120 W. 45 Street, New York, New York 10036, United States., Moraca F; Schrödinger, Inc., 120 W. 45 Street, New York, New York 10036, United States., Li K; Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States., Perkowski AJ; Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States., Ramesh R; Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States., Bowler MM; Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States., Tracy W; Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States., Feher VA; Schrödinger, Inc., 120 W. 45 Street, New York, New York 10036, United States., Sacchettini JC; Departments of Biochemistry and Biophysics, Texas Agricultural and Mechanical University, College Station, Texas 77843, United States., Gold BS; Department of Microbiology & Immunology, Weill Cornell Medicine, New York, New York 10065, United States., Nathan CF; Department of Microbiology & Immunology, Weill Cornell Medicine, New York, New York 10065, United States.; Department of Medicine, Weill Cornell Medicine, New York, New York 10065, United States., Aubé J; Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2022 Feb 10; Vol. 65 (3), pp. 1996-2022. Date of Electronic Publication: 2022 Jan 19.

Discovery of Benzoylsulfonohydrazides as Potent Inhibitors of the Histone Acetyltransferase KAT6A.

Autor: Leaver DJ, Cleary B, Nguyen N, Priebbenow DL, Lagiakos HR; Cancer Therapeutics CRC , 343 Royal Parade , Parkville , Victoria 3052 , Australia., Sanchez J; Walter and Eliza Hall Institute of Medical Research , 1G Royal Parade , Parkville , Victoria 3052 , Australia.; Department of Medical Biology , University of Melbourne , Parkville , Victoria 3050 , Australia., Xue L; School of Pharmaceutical Sciences , Nanjing Tech University , No. 30 South Puzhu Road , Nanjing 211816 , People's Republic of China., Huang F; School of Pharmaceutical Sciences , Nanjing Tech University , No. 30 South Puzhu Road , Nanjing 211816 , People's Republic of China., Sun Y, Mujumdar P, Mudududdla R, Varghese S, Teguh S, Charman SA, White KL, Katneni K, Cuellar M; Institute for Therapeutics Discovery and Development , University of Minnesota , 717 Delaware Street SE , Minneapolis , Minnesota 55455 , United States., Strasser JM; Institute for Therapeutics Discovery and Development , University of Minnesota , 717 Delaware Street SE , Minneapolis , Minnesota 55455 , United States., Dahlin JL; Department of Pathology , Brigham and Women's Hospital, Boston , 75 Francis Street , Boston , Massachusetts 02115 , United States., Walters MA; Institute for Therapeutics Discovery and Development , University of Minnesota , 717 Delaware Street SE , Minneapolis , Minnesota 55455 , United States., Street IP; Walter and Eliza Hall Institute of Medical Research , 1G Royal Parade , Parkville , Victoria 3052 , Australia.; Cancer Therapeutics CRC , 343 Royal Parade , Parkville , Victoria 3052 , Australia.; Department of Medical Biology , University of Melbourne , Parkville , Victoria 3050 , Australia., Monahan BJ; Walter and Eliza Hall Institute of Medical Research , 1G Royal Parade , Parkville , Victoria 3052 , Australia.; Cancer Therapeutics CRC , 343 Royal Parade , Parkville , Victoria 3052 , Australia.; Department of Medical Biology , University of Melbourne , Parkville , Victoria 3050 , Australia., Jarman KE; Walter and Eliza Hall Institute of Medical Research , 1G Royal Parade , Parkville , Victoria 3052 , Australia.; Department of Medical Biology , University of Melbourne , Parkville , Victoria 3050 , Australia., Sabroux HJ; Walter and Eliza Hall Institute of Medical Research , 1G Royal Parade , Parkville , Victoria 3052 , Australia.; Department of Medical Biology , University of Melbourne , Parkville , Victoria 3050 , Australia., Falk H; Walter and Eliza Hall Institute of Medical Research , 1G Royal Parade , Parkville , Victoria 3052 , Australia.; Cancer Therapeutics CRC , 343 Royal Parade , Parkville , Victoria 3052 , Australia.; Department of Medical Biology , University of Melbourne , Parkville , Victoria 3050 , Australia., Chung MC; ACRF Rational Drug Discovery Centre , St. Vincent's Institute of Medical Research , Fitzroy , Victoria 3065 , Australia., Hermans SJ; ACRF Rational Drug Discovery Centre , St. Vincent's Institute of Medical Research , Fitzroy , Victoria 3065 , Australia., Parker MW; ACRF Rational Drug Discovery Centre , St. Vincent's Institute of Medical Research , Fitzroy , Victoria 3065 , Australia., Thomas T; Walter and Eliza Hall Institute of Medical Research , 1G Royal Parade , Parkville , Victoria 3052 , Australia.; Department of Medical Biology , University of Melbourne , Parkville , Victoria 3050 , Australia., Baell JB; School of Pharmaceutical Sciences , Nanjing Tech University , No. 30 South Puzhu Road , Nanjing 211816 , People's Republic of China.; ARC Centre for Fragment-Based Design , Monash University , Parkville , Victoria 3052 , Australia.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2019 Aug 08; Vol. 62 (15), pp. 7146-7159. Date of Electronic Publication: 2019 Jul 17.

A mild method for the efficient [3,3]-sigmatropic rearrangement of N,O-diacylhydroxylamines.

Autor: Lagiakos HR; Monash University, Clayton, Victoria, 3800, Australia., Aguilar MI, Perlmutter P

Publikováno v: The Journal of organic chemistry [J Org Chem] 2009 Oct 16; Vol. 74 (20), pp. 8001-3.