Výsledky vyhledávání - "Vijay Baichwal"

Abstract 4634: Identifying and analyzing tumor subtypes using custom morphology markers for NanoString® GeoMx® Digital Spatial Profiler

Autor: Jessica Runyon, Vijay Baichwal, Weston Stauffer, Christian Nievera

Publikováno v: Cancer Research. 83:4634-4634

Molecular subtyping studies have allowed the allocation of cancer into groups based on similar molecular, morphological, and clinical characteristics. Such studies are critical to help researchers identify actionable targets for drug design and bioma

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::365c122b1902387ee4cf3faa7fa9e9f2
https://doi.org/10.1158/1538-7445.am2023-4634

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Discovery of (2S)-1-[4-(2-{6-Amino-8-[(6-bromo-1,3-benzodioxol-5-yl)sulfanyl]-9H-purin-9-yl}ethyl)piperidin-1-yl]-2-hydroxypropan-1-one (MPC-3100), a Purine-Based Hsp90 Inhibitor

Autor: Damon I. Papac, Rena McKinnon, Ashok C. Bajji, Vijay Baichwal, Rosann Robinson, Richard Trovato, Daniel Wettstein, Paul L. Bartel, Rajendra P. Tangallapally, Kraig M. Yager, Daniel M. Cimbora, Robert O. Carlson, Se-Ho Kim, Mark D. Shenderovich, Benjamin Markovitz

Publikováno v: Journal of Medicinal Chemistry. 55:7480-7501

Modulation of Hsp90 (heat shock protein 90) function has been recognized as an attractive approach for cancer treatment, since many cancer cells depend on Hsp90 to maintain cellular homeostasis. This has spurred the search for small-molecule Hsp90 in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::18136cca1711f48a4a8674ad293c17c9
https://doi.org/10.1021/jm3004619

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Triterpene based compounds with potent anti-maturation activity against HIV-1

Autor: Rena McKinnon, In Chul Kim, Vijay Baichwal, Harry Austin, Esther Arranz-Plaza, Kraig M. Yager, David Gerrish, Dange Vijay Kumar, Mark B. Anderson, Jennifer E. Garrus, Robert O. Carlson, Michael Saunders

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 18:6377-6380

Efforts towards developing orally bioavailable HIV-1 maturation inhibitors starting from betulinic acid 1 are described. SAR resulted in improved potency, physicochemical properties, and enhanced oral absorption in rats.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::09cdc69898aa6a2bf095e6e1f80061f1
https://doi.org/10.1016/j.bmcl.2008.10.098

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Discovery of 2-Chloro-N-(4-methoxyphenyl)-N-methylquinazolin-4-amine (EP128265, MPI-0441138) as a Potent Inducer of Apoptosis with High In Vivo Activity

Autor: John Drewe, Kevin Jessing, Raouf A. Hussain, Christopher M. Pleiman, Khanh C. Hoang, Nilantha Sudath Sirisoma, Songchun Jiang, Gary Mather, Hong Zhang, Azra Pervin, Ben Tseng, Vijay Baichwal, Shailaja Kasibhatla, J. Adam Willardsen, Sui Xiong Cai, Mark B. Anderson

Publikováno v: Journal of Medicinal Chemistry. 51:4771-4779

Using a live cell, high-throughput caspase-3 activator assay, we have identified a novel series of 4-anilinoquinazolines as inducers of apoptosis. In this report, we discuss the discovery of 2-chloro-N-(4-methoxyphenyl)-N-methylquinazolin-4-amine, co

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d961ca79c09484fddbd547986ecdef31
https://doi.org/10.1021/jm8003653

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MPC-6827: A Small-Molecule Inhibitor of Microtubule Formation That Is Not a Substrate for Multidrug Resistance Pumps

Autor: Bruce J. Roth, Nilantha Sudath Sirisoma, Robert O. Carlson, Azra Pervin, Vijay Baichwal, Ira Skvortsova, Shailaja Kasibhatla, Ben Tseng, Sergej Skvortsov, John Drewe, Sui Xiong Cai, Peter Lukas, Christopher M. Pleiman, Nicole English

Publikováno v: Cancer Research. 67:5865-5871

A novel series of 4-arylaminoquinazolines were identified from a cell-based screening assay as potent apoptosis inducers. Through structure-activity relationship studies, MPC-6827 and its close structural analogue, MPI-0441138, were discovered as pro

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a07a3b21402d8c1ce99865b8af94d429
https://doi.org/10.1158/0008-5472.can-07-0127

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Discovery of an L-alanine ester prodrug of the Hsp90 inhibitor, MPC-3100

Autor: Se-Ho Kim, Damon I. Papac, Robert W. Carlson, Rajendra Tangallapally, In Chul Kim, Kraig M. Yager, Chad Bradford, Richard Trovato, Leslie Reeves, Daniel P. Parker, J. Scott Patton, Vijay Baichwal, Ashok C. Bajji, Daniel Wettstein

Publikováno v: Bioorganicmedicinal chemistry letters. 25(22)

Various types of Hsp90 inhibitors have been and continue to undergo clinical investigation. One development candidate is the purine-based, synthetic Hsp90 inhibitor 1 (MPC-3100), which successfully completed a phase I clinical study. However, further

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1bba84eb10c356e88bbe6233c942d584
https://pubmed.ncbi.nlm.nih.gov/26483201

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Hydrophilic, Pro-Drug Analogues of T138067 Are Efficacious in Controlling Tumor Growth In Vivo and Show a Decreased Ability To Cross the Blood Brain Barrier

Autor: Susan Schwender, Holger Beckmann, David Clark, Martin Thoolen, Vijay Baichwal, Walter Frankmoelle, Steven M. Rubenstein, Daniel Roche, Juan C. Jaen, Qiuping Ye, Edit Santha

Publikováno v: Journal of Medicinal Chemistry. 44:3599-3605

The novel anticancer compound T138067 is an irreversible inhibitor of tubulin polymerization. Amides 3-6 were synthesized using standard methodologies and determined to be significantly less lipophilic than T138067 based on logP calculations. Tubulin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4966339f1b9eba9b6b13058fe4314baa
https://doi.org/10.1021/jm000478d

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