Periodic Reporting for period 1 - STTDAA (Synthesis of Truncated Tirandamycin A-D Derivatives as new Antihelminthic Agents)
Reporting period: 2015-06-01 to 2017-05-31
It is reported that tirandamycin B, a natural product, inhibits asparagine-tRNA synthetase (AsnRS) from B. malayi (one out of three types of roundworm casing LF), kills the adult B. malayi parasite, and does not exhibit significant general cytotoxicity to human hepatic cells.
The project has resulted in development of efficient synthetic strategies for the preparation of truncated tirandamycin derivatives with a scaffold that retains the structural integrity of the natural product.
The synthetic developments have been guided by computational chemistry (docking; month 12-20) and in part biological testing (still ongoing; month 20-24).
A manuscript based on the results generated by the researcher Dr. Tania Jiménez throughout the project will be submitted (manuscript in preparation) to a high impact journal (e.g. Angewant Chemie) as soon as the biological evaluation of the truncated tirandamycin derivatives are completed.
Parts of the results have been presented at international research conferences: Bienal de quimica organica in Huelva, Spain (14-17 June 2016), The SISOC XI in Basque Country (13-15 July 2016) and ACS international conference in San Francisco, USA (3-6 April 2017).
In addition the researcher has completed a training program, that included learning new techniques (e.g. how to run enzymatic assays and carry out docking), project management, leadership training (being responsible for two graduate students) and gaining skills such as motivating others, communication, reviewing progress, applying practical strategies to get the best from a research team, getting and managing finances, writing papers, projects and grant proposals, and presenting scientific results. The researcher has been involved in the organization and implementation of the annual ¨day of open door¨ aiming at closing the gap between academia and the broad public and at demonstrating the impact of research on innovation, prosperity and public welfare. She had also given science master-classes during the Annual High School Days and had participated in the organization of the faculty´s job fair.
The researcher had gained a strong scientific independency and general academic maturity, and thereby had enhanced and maximized her contribution to the European knowledge-based economy and society.