Investigation of 3′-debenzoyl-3′-(3-([124I]-iodobenzoyl))paclitaxel analog as a radio-tracer to study multidrug resistance in vivo

Autor: Gunda I. Georg, Ralph J. Bernacki, J. M. Veith, N. D. Chaudhary, M. Abouzied, Rutao Yao, Munawwar Sajjad, U. Riaz, Hani A. Nabi, D. A. Erb

Publikováno v: Applied Radiation and Isotopes. 70:1624-1631

A study was carried out to identify a suitable radioactive paclitaxel analog and to use it to investigate tumor multidrug resistance in vivo. 3'-Debenzoyl-3'-(3-([(124)I]-iodobenzoyl))paclitaxel was prepared by aromatic iodination of 3'-debenzoyl-3'-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::fe22f843831fadfa68b695a8670d3b97
https://doi.org/10.1016/j.apradiso.2012.03.008

Design, Synthesis, and Biological Evaluation of New-Generation Taxoids

Autor: Ilaria Zanardi, Jon Mallen-St. Clair, Iwao Ojima, Susan Band Horwitz, Shujun Xia, Xianrui Zhao, Dafna Bar-Sagi, David Gallager, Jin Chen, Tao Wang, Xudong Geng, Michael L. Miller, Ralph J. Bernacki, Larisa V. Kuznetsova, Songnian Lin, Jean M. Veith, Jennifer L. Guerriero, Chuanxing Qu, Liang Sun, Christopher P. Borella, Paula Pera

Publikováno v: Journal of Medicinal Chemistry. 51:3203-3221

Novel second-generation taxoids with systematic modifications at the C2, C10, and C3'N positions were synthesized and their structure-activity relationships studied. A number of these taxoids exhibited exceptionally high potency against multidrug-res

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b2d811bbf1dba302b8e6afa428c01a96
https://doi.org/10.1021/jm800086e

The 4′-O-benzylated doxorubicin analog WP744 overcomes resistance mediated by P-glycoprotein, multidrug resistance protein and breast cancer resistance protein in cell lines and acute myeloid leukemia cells

Autor: Laurie A. Ford, Tracy A. Brooks, Hans Minderman, Maria R. Baer, Brian N. Bundy, Michael R. Vredenburg, Ralph J. Bernacki, Waldemar Priebe, Kieran L. O’Loughlin

Publikováno v: Investigational New Drugs. 25:115-122

Background: The synthetic 4’-O-benzylated doxorubicin analog WP744 was designed to abrogate transport by the multidrug resistance (MDR)-associated ATP-binding cassette (ABC) proteins P-glycoprotein (Pgp) and multidrug resistance protein (MRP-1). We

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5f9d7bf2730d1e5f3a92567b20771689
https://doi.org/10.1007/s10637-006-9018-3

Improved Synthesis of β-D-6-Methylpurine Riboside and Antitumor Effects of the β-D- and α-D-Anomers

Autor: Ralph J. Bernacki, Paula Pera, Janice R. Sufrin, Arthur J. Spiess, Canio J. Marasco

Publikováno v: Molecules, Vol 10, Iss 8, Pp 1015-1020 (2005)
Molecules
Volume 10
Issue 8
Pages 1015-1020
Molecules : A Journal of Synthetic Chemistry and Natural Product Chemistry

6-Methylpurine-beta-D-riboside (beta-D-MPR) has been synthesized by coupling 6-methylpurine and 1-O-acetyl-2,3,5-tri-O-benzoyl-D-ribose using conditions that produce the beta-D-anomer exclusively. The in vitro antitumor effects of beta-D-MPR and 6-me

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e99f764d7cfdda1fcc9dd8eeb6f7d5f4
https://doi.org/10.3390/10081015

Design and synthesis of de novo cytotoxic alkaloids through mimicking taxoid skeleton

Autor: Ralph J. Bernacki, Paula Pera, Iwao Ojima, Xudong Geng, Raphaël Geney

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 14:3491-3494

Based on a common pharmacophore model and the hypothesis that the baccatin core of taxoids is a scaffold securing the proper orientation of the side chains, a bicyclic alkaloid scaffold was designed as a baccatin surrogate. Using this scaffold, two n

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bbf3ba680a10419ae81eb1876bf05e30
https://doi.org/10.1016/j.bmcl.2004.04.060