Zobrazeno 1 - 10
of 52
pro vyhledávání: '"Nareshkumar F. Jain"'
Publikováno v:
Pharmaceutical Research
The list of ADCs in the clinic continues to grow, bolstered by the success of first two marketed ADCs: ADCETRIS® and Kadcyla®. Currently, there are 40 ADCs in various phases of clinical development. However, only 34 of these have published their st
Autor:
Dmitry Borkin, Jagath Reddy Junutula, Jianqing Huang, Nareshkumar F. Jain, Jennifer Lu, Ying-Ping Jiang, Vasu Jammalamadaka, Sean W. Smith, Sylvia J. Degrado, Jianyu Zhu
Publikováno v:
ACS medicinal chemistry letters. 9(1)
Antibody–drug conjugates (ADCs) represent an important class of emerging cancer therapeutics. Recent ADC development efforts highlighted the use of pyrrolobenzodiazepine (PBD) dimer payload for the treatment of several cancers. We identified the is
Autor:
Sylvia Degrado, Kimberly D. Klarmann, Dimiter S. Dimitrov, Julia Scheiermann, Brad St. Croix, Zhongyu Zhu, Dmitry Borkin, Yang Feng, Steven Seaman, Mi Young Yang, Enrique Zudaire, Holly Morris, Yanping Wang, Nareshkumar F. Jain, Karen Morris, Jinyu Li, Mary Beth Hilton, Sean W. Smith, Jonathan R. Keller, Lino Tessarollo, Saurabh Saha, Christopher S. Szot, Amit Chaudhary, Deborah A. Swing, Xiaoyan M. Zhang, Decrescenzo Gary A, Dean Welsch
Publikováno v:
Cancer cell. 31(4)
Targeting the tumor vasculature with antibody-drug conjugates (ADCs) is a promising anti-cancer strategy that in order to be realized must overcome several obstacles, including identification of suitable targets and optimal warheads. Here, we demonst
Autor:
Dominique Depré, Wim Albert Alex Aelterman, Zhihua Sui, Xun Li, Dominic Ormerod, Andras Horvath, Nareshkumar F. Jain, Ronald K. Russell
Publikováno v:
Organic Process Research & Development. 13:102-105
A novel and economical process was developed for recycling the undesired enantiomer, (S)-2,8-dimethoxy-5-{4-[2-(1-piperidinyl)ethoxy]phenyl}-11,12-dihydro-5H-6,13-dioxabenzo[3,4]cyclohepta[1,2-a]naphthalene (1b) obtained from chiral chromatographic s
Autor:
Nareshkumar F. Jain, Xin Chen, Pamela Tannenbaum, Zhihua Sui, Fu-An Kang, Scott G. Lundeen, George F. Allan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:3687-3690
Replacement of the 7-CH2 group of natural steroid with an oxygen atom led to identification of unnatural 7-oxa-steroids as potent and selective progesterone receptor antagonists. The unnatural 7-oxa-steroids exhibited a different structure–activity
Autor:
Shawn Branum, Ramesh M. Kanojia, Xun Li, Robert Ma, Ronald K. Russell, Nareshkumar F. Jain, Scott Youells, Sandra Beish, Richard E. Adams, Michael Reuman, Zhihua Sui, Jerry R. Roberts
Publikováno v:
Organic Process Research & Development. 11:414-421
Unsymmetrical benzopyranobenzopyran compounds are novel selective estrogen receptor modulators (SERMs). A reproducible and nonchromatographic process was developed to prepare multihundred gram quan...
Autor:
George F. Allan, Peifang Zhu, Joseph W. Gunnet, Olivia Linton, Nareshkumar F. Jain, Keith T. Demarest, Scott G. Lundeen, Jihua Guan, Pamela Tannenbaum, Xin Chen, Fu-An Kang, Jun Xu, Zhihua Sui
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:907-910
A novel series of oxa-steroids 6 derived from (8S, 13S, 14R)-7-oxa-estra-4,9-diene-3,17-dione 1 have been synthesized and identified as potent and selective progesterone receptor antagonists. These novel oxa-steroids showed similar potency to mifepri
Publikováno v:
Tetrahedron Letters. 48:193-197
The first enantioselective synthesis of (8 S ,13 S ,14 R )-7-oxa-estra-4,9-diene-3,17-dione with the trans -C/D ring junction is described. Key features of the synthesis include Ag 2 O-mediated C–O bond formation, thermodynamically controlled axial
Publikováno v:
Tetrahedron Letters. 47:9021-9024
The first synthesis of a novel oxa-steroid, rac-(8R,13S,14S)-7-oxa-estra-4,9-diene-3,17-dione has been achieved via stereoselective catalytic hydrogenation of the tetra-substituted indene intermediate, whose structure was confirmed by X-ray crystallo
Autor:
Zhihua Sui, Ronald K. Russell, Ningyi Chen, Michael Reuman, Nareshkumar F. Jain, Jiayi Xu, Xun Li
Publikováno v:
Tetrahedron Letters. 47:5909-5913
Various substituents were introduced onto the methyl group in 4-methyl coumarins through lithiation, followed by reactions with a wide range of electrophiles. The presence of an alkoxy group on 6′-phenyl ring was found to be pivotal for the success