Author: Dömling, Alexander ; Agarwal, Seema ; Schauer-Vukašinović, Vesna ; Kaur, Gurmeet ; Holbeck, Susan ; Hollingshead, Melinda ; Camalier, Richard F.

Tubulysin A (tubA) is a natural product isolated from a strain of myxobacteria that has been shown to depolymerize microtubules and induce mitotic arrest. The potential of tubA as an anticancer and antiangiogenic agent is explored in the present study. tubA shows potent antiproliferative activity in a panel of human cancer cell lines irrespective of their multidrug resistance properties. It induces apoptosis in cancer cells but not in normal cells and shows significant potential antiangiogenic properties in several in vitro assays. It is efficacious in initial animal studies using a hollow fibre assay with 12 different human tumour cell lines. This study suggests that both in vitro and preclinical profiles of tubA may translate into clinically useful anticancer properties.

01 Mar 2006·Bioorganic & Medicinal Chemistry LettersQ4 · MEDICINE

Design and modular parallel synthesis of a MCR derived α-helix mimetic protein–protein interaction inhibitor scaffold

Q4 · MEDICINE

Article

Author: Yingchun Lu ; Vesna Schauer-Vukašinović ; Sukumar Sakamuri ; Sanjay Menon ; Quin-Zene Chen ; Walfrido Antuch ; Alexander Dömling ; Seema Agarwal ; Barbara Beck ; Sibylle Hess

A terphenyl alpha-helix mimetic scaffold recognized to be capable of disrupting protein-protein interactions was structurally morphed into an easily amenable and versatile multicomponent reaction (MCR) backbone. The design, modular in-parallel library synthesis, initial cell based biological data, and preliminary in vitro screening for the disruption of the Bcl-w/Bak protein-protein interaction by representatives of the MCR derived scaffold are presented.

01 Feb 2006·Letters in Drug Design & Discovery

Initial Design and Synthesis of Conformationally Restricted and Pharmacophore-Based Scaffold Hopping Analogs of a Ras Pathway Modulator and Evaluation of Their MAPK Inhibitory Activities

Author: Khazak, Vladimir ; Menon, Sanjay R. ; Chen, Quin-Zene ; Lu, Yingchun ; Weber, Lutz ; Sakamuri, Sukumar ; Schabbert, Silke ; Keng, Yen-Fang ; Illgen, Katrin

The initial design and synthesis of conformationally restricted and pharmacophore-based scaffold hopping analogs of a Ras/Raf protein interaction inhibitor were undertaken with the objective of identifying alternate chem. scaffolds exhibiting similar biol. activities.Evaluation of the MAPK pathway signaling inhibitory activity and antiproliferative activity of the synthesized derivatives was performed.

100 Deals associated with Morphochem AG

100 Translational Medicine associated with Morphochem AG

Corporation Tree

Boost your research with our corporation tree data.

view full example data

Pipeline

Pipeline Snapshot as of 24 Jan 2025

No data posted

Deal

Boost your decision using our deal data.

view full example data

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Profit

Explore the financial positions of over 360K organizations with Synapse.

view full example data

Grant & Funding(NIH)

Access more than 2 million grant and funding information to elevate your research journey.

view full example data

Investment

Gain insights on the latest company investments from start-ups to established corporations.

view full example data

Financing

Unearth financing trends to validate and advance investment opportunities.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis

Morphochem AG

Overview

Related

Corporation Tree

Pipeline

Pipeline Snapshot as of 24 Jan 2025

Deal

Translational Medicine

Profit

Grant & Funding(NIH)

Investment

Financing