Therapies from Thiopeptides

Author:

Hwang Hee-Jong12ORCID,Ciufolini Marco A.1

Affiliation:

1. Department of Chemistry, The University of British Columbia, 2036 Main Mall, Vancouver, BC V6T 1Z1, Canada

2. A&J Science, Ltd., 80 Chumbok Ro, Dong Gu, Daegu 41061, Republic of Korea

Abstract

The first part of this contribution describes solutions that were developed to achieve progressively more efficient syntheses of the thiopeptide natural products, micrococcins P1 and P2 (MP1–MP2), with an eye toward exploring their potential as a source of new antibiotics. Such efforts enabled investigations on the medicinal chemistry of those antibiotics, and inspired the development of the kinase inhibitor, Masitinib®, two candidate oncology drugs, and new antibacterial agents. The studies that produced such therapeutic resources are detailed in the second part. True to the theme of this issue, “Organic Synthesis and Medicinal Chemistry: Two Inseparable Partners”, an important message is that the above advances would have never materialized without the support of curiosity-driven, academic synthetic organic chemistry: a beleaguered science that nonetheless has been—and continues to be—instrumental to progress in the biomedical field.

Funder

NIH

NSF

NSERC

Canada Research Chair

University of British Columbia

AB Science SA, Paris, France

IMERA

A&J Science, Daegu, Republic of Korea

Korea Health Technology R&D Project

Publisher

MDPI AG

Subject

Chemistry (miscellaneous),Analytical Chemistry,Organic Chemistry,Physical and Theoretical Chemistry,Molecular Medicine,Drug Discovery,Pharmaceutical Science

Reference54 articles.

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