Runtao Li

TL;DR: A series of 4(3H)-quinazolinone derivatives with dithiocarbamate side chains were synthesized and tested for their in vitro antitumor activity against human myelogenous leukemia K562 cells, and Piperazine-1-carbodithioate 8q exhibited significant inhibitory activity.

TL;DR: A new covalent docking package, the CovalentDock, built on the top of the source code of Autodock, which is compatible with existing scoring functions used in docking, while handling the molecular geometry constrains of the covalENT linkage with special atom types and directional grid maps.

TL;DR: Increase in the polarity and/or introduction of suitable acyl groups at the 4-N atom of the lead compound 4 are favorable for the improvement of activity.

TL;DR: The l -proline-based dipeptide has been developed as an efficient catalyst for the direct asymmetric aldol reactions of unmodified ketones with various aldehydes including aromatic, aliphatic, hetero-aromatic, and unsaturated aldehyde as discussed by the authors.

TL;DR: The first direct organocatalytic asymmetric vinylogous Michael addition reactions of gamma-butenolides to chalcones have been developed by using chiral 1,2-diaminocyclohexane as a novel organoc atalyst via a di-iminium transition state to provide syn-Michael products with good yields and high diastereoselectivities.