Macromolecular Drug Conjugates, Metronidazole-Cyclodextrin Prodrugs

2012 ◽  
Author(s):  
Zhizhong Wang ◽  
Mengying Liu
Keyword(s):  
Drug Conjugates ◽  
Macromolecular Drug

scholarly journals Synthesis and in vivo anticancer evaluation of poly(organo)phosphazene-based metallodrug conjugates

2017 ◽  
Vol 46 (36) ◽  
pp. 12114-12124 ◽  
Author(s):  
Carmen M. Hackl ◽  
Beatrix Schoenhacker-Alte ◽  
Matthias H. M. Klose ◽  
Helena Henke ◽  
Maria S. Legina ◽  
...  
Keyword(s):  
Side Effects ◽  
Tumor Growth ◽  
Drug Conjugates ◽  
Polymer Conjugation ◽  
Local Side ◽  
Macromolecular Drug

Macromolecular drug conjugates: Polymer conjugation reduces local side effects and tumor growth in vivo.

Macromolecular Drug Conjugates II. Metronidazole-Dextran Prodrugs

1993 ◽  
Vol 8 (4) ◽  
pp. 383-392 ◽  
Author(s):  
Georgeta Mocanu ◽  
Anton Airinei ◽  
Adrian Carpov
Keyword(s):  
Drug Conjugates ◽  
Dextran Prodrugs ◽  
Macromolecular Drug

Macromolecular-Drug Conjugates Nalidixic Acid and Oxacillin Dextran

2000 ◽  
Vol 15 (3) ◽  
pp. 245-256 ◽  
Author(s):  
DOINA MIHAI ◽  
GEORGETA MOCANU ◽  
ADRIAN CARPOV
Keyword(s):  
Nalidixic Acid ◽  
Drug Conjugates ◽  
Macromolecular Drug

Macromolecular-Drug Conjugates—Nalidixic Acid and Oxacillin-Dextran

2000 ◽  
Vol 15 (3) ◽  
pp. 245-256
Author(s):  
Doina Mihai ◽  
Georgeta Mocanu ◽  
Adrian Carpov
Keyword(s):  
Nalidixic Acid ◽  
Drug Conjugates ◽  
Macromolecular Drug

Macromolecular drug conjugates. V. Theophylline-dextran

1996 ◽  
Vol 40 (1-2) ◽  
pp. 1-9 ◽  
Author(s):  
Georgeta Mocanu ◽  
A. Airinei ◽  
A. Carpov
Keyword(s):  
Drug Conjugates ◽  
Macromolecular Drug

ASCO-GU 2019: Metastasierte Urothelkarzinome

2019 ◽  
Vol 10 (03) ◽  
pp. 140-141
Author(s):  
Alexander Kretzschmar
Keyword(s):  
San Francisco ◽  
Antibody Drug Conjugates ◽  
Drug Conjugates ◽  
Chapel Hill ◽  
Antibody Drug

Die Therapielandschaft des metastasierten Urothelkarzinoms hat sich seit der Zulassung der ersten Immun-Checkpoint-Inhibitoren verändert. Die neuen Therapien sind deutlich effektiver, allerdings erreichen die Responseraten der neuen Therapien nur bis zu etwa 30 %, beklagte Prof. Matthew Milowsky, Chapel Hill/USA, auf einer Oral Abstract Session auf dem ASCO-GU. In San Francisco gaben erste Vorträge und Poster bereits einen Einblick, wovon diejenigen Patienten profitieren könnten, die auf die etablierten Chemotherapien und die neuen Immuntherapien nicht ansprechen. Manche Onkologen sprechen bereits von der „Post-Checkpoint-Ära”. Als Kandidaten werden vor allem Antikörper-Wirkstoff-Konjugate (antibody-drug conjugates; ADC) gehandelt – und zwar nicht nur zur Therapie des metastasierten Blasenkarzinoms.

Design, 22-step synthesis, and evaluation of highly potent D-ring modified and linker-equipped analogs of spongistatin 1

2018 ◽  
Author(s):  
James Leighton ◽  
Linda M. Suen ◽  
Makeda A. Tekle-Smith ◽  
Kevin S. Williamson ◽  
Joshua R. Infantine ◽  
...  
Keyword(s):  
Targeted Delivery ◽  
Functional Group ◽  
Human Cancer ◽  
Natural Sources ◽  
Spongistatin 1 ◽  
Human Cancer Cell Lines ◽  
Drug Conjugates ◽  
Attractive Candidate ◽  
Complex Fragment ◽  
Antibody Drug

With an average GI50 value against the NCI panel of 60 human cancer cell lines of 0.12 nM, spongistatin 1 is among the most potent anti-proliferative agents ever discovered rendering it an attractive candidate for development as a payload for antibody-drug conjugates and other targeted delivery approaches. It is unavailable from natural sources and its size and complex stereostructure render chemical synthesis highly time- and resource-intensive, however, and its development requires more efficient and step-economical synthetic access. Using novel and uniquely enabling direct complex fragment coupling alkallyl- and crotylsilylation reactions, we have developed a 22-step synthesis of a rationally designed D-ring modified analog of spongistatin 1 that is equipotent with the natural product, and have used that synthesis to establish that the C(15) acetate may be replaced with a linker functional group-bearing ester with only minimal reductions in potency.<br><div><br></div>

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