Antibody-drug conjugates (ADCs) represent a promising cancer therapy modality which
specifically delivers highly toxic payloads to cancer cells through antigen-specific …

Drug conjugates are obtained from tumor-located vectors connected to cytotoxic agents via
linkers, which are designed to deliver hyper-toxic payloads directly to targeted cancer cells …

Filling a gap on the market, this handbook and ready reference is unique in its discussion of
the usefulness of various heterocyclic systems in the synthesis of natural products. Clearly …

The synthesis of a new generation of highly cytotoxic tubulysin analogues (ie, tubugis) is
described. In the key step, the rare, unstable, and synthetically difficult to introduce tertiary …

A streamlined total synthesis of N 14-desacetoxytubulysin H (Tb1) based on a C–H
activation strategy and a short total synthesis of pretubulysin D (PTb-D43) are described …

N4-Phenyl 2-acetylpyridine thiosemicarbazone (H2Ac4Ph; N-(phenyl)-2-(1-(pyridin-2-yl)
ethylidene) hydrazinecarbothioamide) and its N4-ortho-,-meta-and-para-fluorophenyl …

Covering: 2000 to 2014 Since their first report in 2000, tubulysins have sparked great
interest for development as anti-cancer agents due to their exceptionally potent …

Based on classical colchicine site ligands and a computational model of the colchicine
binding site on beta tubulin, two classes of chalcone derivatives were designed, synthesized …

Improved, streamlined total syntheses of natural tubulysins such as V (Tb45) and U (Tb46)
and pretubulysin D (PTb-D43), and their application to the synthesis of designed tubulysin …

A concise and modular total synthesis of the highly potent N14-desacetoxytubulysin H (1)
has been accomplished in 18 steps in an overall yield of up to 30%. Our work highlights the …